Compounds useful for the treatment of disorders and methods related thereto

Compounds of Formula (I) are developed to treat mental and neurological disorders by targeting brain alterations and dysfunction, providing therapeutic benefits for conditions such as depressive disorders and anxiety disorders.

WO2026015507A1PCT designated stage Publication Date: 2026-01-15OTSUKA AMERICA PHARMACEUTICAL INC
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Patent Information

Application Number
PCT/US2025/036756
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2025-05-22
Filing Date
2025-07-08
Publication Date
2026-01-15

AI Technical Summary

Technical Problem

There is a need for the development of additional effective treatments for mental health disorders and neurological disorders, including depressive disorders, anxiety disorders, schizophrenia, eating disorders, post-traumatic stress disorder, attention deficit/hyperactivity disorder, and obsessive-compulsive disorder, among others, due to alterations, dysfunction, and/or damage to the brain.

Method used

The development of compounds of Formula (I) or their stereoisomers, pharmaceutically acceptable salts, solvates, and/or prodrugs, with specific structural variations in R1 to R19, which are designed to target these disorders.

Benefits of technology

The compounds of Formula (I) demonstrate potential therapeutic effects in treating a range of mental and neurological disorders, including depressive disorders, anxiety disorders, and neurodegenerative disorders, by addressing brain alterations and dysfunction.

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Abstract

The present disclosure relates to compounds of general Formula (I), to processes for their preparation, and to their use for treating diseases, disorders, or conditions. The diseases, disorders, or conditions include, for example, mental illnesses and neurological disorders.
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Description

COMPOUNDS USEFUL FOR THE TREATMENT OF DISORDERS AND METHODS RELATED THERETOCROSS-REFERENCE TO RELATED APPLICATION(S) AND CLAIM OF PRIORITY

[0001] This application claims the benefit of priority of U.S. Provisional Application Nos. 63 / 668,448 and 63 / 810,258 filed in the U.S. Patent & Trademark Office on July 8, 2024 and May 22, 2025, respectively, the complete disclosures of which are incorporated herein by reference.FIELD

[0002] The application relates to compounds of general Formula (I), and methods of using such compounds, including methods for the treatment of different diseases, disorders, and conditions, including, for example, mental illnesses and neurological diseases, disorders, and conditions in the fields of psychiatry, neurobiology, and pharmacotherapy, among others.BACKGROUND

[0003] Mental health disorders, or mental illnesses, refer to a wide range of disorders that include, but are not limited to, depressive disorders, anxiety and panic disorders, schizophrenia, eating disorders, substance misuse disorders, post-traumatic stress disorder, attention deficit / hyperactivity disorder, and obsessive-compulsive disorder. Many mental health disorders, as well as neurological disorders, are impacted by alterations, dysfunction, degeneration, and / or damage to the brain.

[0004] There is a need in the art for development of compounds for additional effective treatments for the above and other diseases, disorders, and conditions discussed herein.SUMMARY

[0005] This Summary is provided to introduce a selection of representative concepts in a simplified form, which representative concepts are further described below in the Detailed Description. This Summary is not necessarily intended to identify key features or essential features of the claimed subject matter, nor is it or the objects and benefits described herein intended to be used to limit the scope of the claimed subject matter.

[0006] The present application includes one or more compounds of Formula (I) or a stereoisomer thereof:or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof, wherein:X is CR18R19, O, S(O), S(O)2, or S;R1is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C3- C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl;R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneOC1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC3-C6cycloalkyl, optionally substituted OC1- C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1- C6alkylene(5- to 6-membered) heteroaryl, or R2and R3are linked to one another to form an O- (CH2)1-2-O- linkage;R3is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl, or R3and R2are linked to one another to form the O-(CH2)1-2-O- linkage;R4is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl;R5is selected from H, D, halo, and optionally substituted C1-C6alkyl;R6is selected from H, D, halo, and optionally substituted C1-C6alkyl;R7is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl;Q is selected from:over a bond means that the bond is attached to a remaining portion of the compound; each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R10is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R13is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R15is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;R16and R17are included in a structurein which R16is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl, and R17is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl; ortogether form a carbonyl group having a structureR18is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl;R19is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl; m is 0, 1, or 2; n is 0, 1 , or 2; o is 0, 1 , or 2; p is 0, 1 , or 2; one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective alternative isotopes thereof;provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, CH3, and OCH3, R3is selected from H and F, R4is selected from H and F, R5is H, R6is H, R7is H, Q is Q1 , and m is 0, then R9is not H; provided when X is CR18R19, R18is H, R19is selected from H and CH3, R5is CH3, R8is CH3, Q isQ2, R11is selected from H, CH3, CH2CH3,and n is 0, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R5is CH3, R6is CH3, Q is Q2, R11is CH3, n is 1 , and R10is CH3, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, CH2CH3, and OCH3, R3is selected from H and F, R4is H, R5is H, R6is H, R7is H, Q is Q2, and n is 0, then R11is not selected from H and CH3; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, Cl, Br, CH3, and OCH3, R3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, CH3, and OCH3, R5is H, R6is H, R7is H, Q is Q4, R16is H, R17is H, and p is 0, then R15is not H; and the compound of Formula (I) is not selected from the following and stereoisomers thereof:

[0007] In some embodiments, the compound of Formula (I) is not selected from a partially or fully deuterated analog of the following, and / or in some embodiments the compound of Formula (I) is not selected from a partially or fully halogenated analog of compounds selected from:4-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1H-inden-1-yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzothiophene-1 ,1 -dione;3-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro- 1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

[0008] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R5is C1-C4alkyl, R6is C1- C4alkyl, Q is Q2, and n is 0, then R7is not OH.

[0009] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R1is selected from H, Br, and OCH3, R2is selected from H, F, and CH3, R3is H, R4is selected from H and F, R5is CH3, R6is CH3, Q is Q2, R11is selected from H , and n is 0, then R7is not OH.

[0010] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R1is selected from H, F, Cl, Br, CH3, OCH3, OCH2CH3, OiPr, and phenyl, R2is selected from H, F, Cl, Br, CH3,CH2CH3, OCH3, andR3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, and OCH3, R5is CH3, R6is CH3, Q is Q2, R11is selected from CH3, and n is 0, then R7is not OH.

[0011] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from F and CH3, R3is H, R4is H, R5is CH3, R6is CH3, Q is Q2, R11is CH2CH3, and n is 0, then R7is not OH.

[0012] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R5is C1-C6alkyl, R6is C1-C6alkyl, Q is Q2, R11is selected from H and unsubstituted C1-C6alkyl, and n is 0, then R7is not OH.

[0013] In some embodiments, provided when X is CR18R19, R18is H, R19is H, R5is selected from halo and C1-C6alkyl, R6is selected from halo and C1-C6alkyl, Q is Q2, R11is selected from H and optionally substituted C1-C6alkyl, and n is 0, then R7is not OH.

[0014] In some embodiments, provided when X is CR18R19, R18is H, R19is H, Q is Q1 , and m is 0, then R9is not selected from H and CH3.

[0015] In some embodiments, provided when X is CR18R19, R18is H, R19is H, Q is Q2, and n is0, then R11is not selected from H, CH3, CH2CH3,

[0016] In some embodiments, provided when X is CR18R19, R18is H, R19is H, Q is Q3, and o is 0, then R13is not selected from H and CH3.

[0017] In some embodiments, provided when X is CR18R19, R18is H, R19is H, Q is Q4, and p is 0, then R15is not H.

[0018] In some embodiments, provided when X is CR18R19, R18is H, R19is CH3, Q is Q1, and m is 0, then R9is not H.

[0019] In some embodiments, provided when X is CR18R19, R18is H or CH3, R19is CH3, Q is Q2, and n is 0, then R11is not selected from H and CH3.

[0020] In some embodiments, provided when X is O, Q is Q1, and m is 0, then R9is not H.

[0021] In some embodiments, provided when X is O, Q is Q2, and n is 0, then R11is not H.

[0022] In some embodiments, provided when X is 0, Q is Q3, and o is 0, then R13is not H.

[0023] In some embodiments, provided when X is O, Q is Q4, and p is 0, then R15is not H.

[0024] In some embodiments, provided when X is S(O)2, Q is Q1, and m is 0, then R9is not H.

[0025] In some embodiments, provided when X is S(O)2, Q is Q3, and o is 0, then R13is not H.

[0026] In some embodiments, provided when X is S, Q is Q1, and m is 0, then R9is not H.

[0027] In some embodiments, provided when X is S, Q is Q2, and n is 0, then R11is not selected from H and CH3.

[0028] In some embodiments, provided when X is S, Q is Q3, and o is 0, then R13is not H.

[0029] In some embodiments, provided when X is S, Q is Q4, and p is 0, then R15is not H.

[0030] In some embodiments, the present application includes one or more compounds of Formula (I) or a stereoisomer thereof:or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof, wherein:X is CR18R19, O, S(O), S(O)2, or S;R1is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C3- C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl;R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneOC1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC3-C6cycloalkyl, optionally substituted OC1- C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1- C6alkylene(5- to 6-membered) heteroaryl, or R2and R3are linked to one another to form an O- (CH2)1-2-O- linkage;R3is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl, or R3and R2are linked to one another to form the O-(CH2)1-2-O- linkage;R4is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl;R5is selected from H, D, halo, and optionally substituted C1-C6alkyl;R6is selected from H, D, halo, and optionally substituted C1-C6alkyl;R7is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl;Q is selected from:over a bond means that the bond is attached to a remaining portion of the compound; each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R10is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R13is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R15is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;R16and R17are included in a structurein which R16is selected from H, D, halo,OH, and optionally substituted C1-C6alkyl, and R17is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl; ortogether form a carbonyl group having a structureR18is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl;R19is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl; m is 0, 1, or 2; n is 0, 1 , or 2; o is 0, 1 , or 2; p is 0, 1 , or 2; one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective alternative isotopes thereof; and the compound is not selected from the following and stereoisomers thereof:4-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1H-inden-1-yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 -benzofuran-3-yl)methyl]pyrrolidine; and2-[(2,3-dihydro- 1 H-inden-1 -yl)methyl]pyrrolidine.

[0031] In some embodiments, the present application includes one or more compounds of Formula (I) or a stereoisomer thereof:or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof,wherein:X is CR18R19, O, S(O), S(O)2, or S;R1is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C3- C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl;R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneOC1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC3-C6cycloalkyl, optionally substituted OC1- C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1- C6alkylene(5- to 6-membered) heteroaryl, or R2and R3are linked to one another to form an 0- (CH2)1-2-O- linkage;R3is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl, or R3and R2are linked to one another to form the O-(CH2)1-2-O- linkage;R4is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl;R5is selected from H, D, halo, and optionally substituted C1-C6alkyl;R6is selected from H, D, halo, and optionally substituted C1-C6alkyl;R7is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl;Q is selected from:over a bond means that the bond is attached to a remaining portion of the compound; each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R10is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R13is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R15is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;R18and R17are included in a structure, in which R16is selected from H, D, halo,OH, and optionally substituted C1-C6alkyl, and R17is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl; ortogether form a carbonyl group having a structureR18is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl;R19is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl; m is 0, 1, or 2; n is 0, 1 , or 2; o is 0, 1 , or 2; p is 0, 1 , or 2; one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R8, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R18are optionally and independently replaced with one or more respective alternative isotopes thereof;provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, CH3, and OCH3, R3is selected from H and F, R4is selected from H and F, R5is H, R6is H, R7is H, Q is Q1 , and m is 0, then R9is not H; provided when X is CR18R19, R18is H, R19is H, R1is selected from H, Br, and OCH3, R2is selected from H, F, and CH3, R3is H, R4is selected from H and F, R5is CH3, R6is CH3, Q is Q2, R11is selected from H , and n is 0, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is selected from H, F, Cl, Br, CH3, OCH3,OCH2CH3, OiPr, and phenyl, R2is selected from H, F, Cl, Br, CH3, CH2CH3, OCH3, andR3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, and OCH3, R5is CH3, R6is CH3, Q is Q2, R11is selected from CH3, and n is 0, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from F and CH3, R3is H, R4is H, R5is CH3, R6is CH3, Q is Q2, R11is CH2CH3, and n is 0, then R7is not OH. provided when X is CR18R19, R18is H, R19is H, R5is CH3, R6is CH3, Q is Q2, R11is CH3, n is 1 , and R10is CH3, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, CH2CH3, and OCH3, R3is selected from H and F, R4is H, R5is H, R6is H, R7is H, Q is Q2, and n is 0, then R11is not selected from H and CH3; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, Cl, Br, CH3, and OCH3, R3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, CH3, and OCH3, R5is H, R6is H, R7is H, Q is Q4, R16is H, R17is H, and p is 0, then R15is not H; and the compound of Formula (I) is not selected from the following and stereoisomers thereof:4-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1H-inden-1-yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2 ,3-di hyd robenzofu ran-3-y I ) py rro I id ine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihyd robenzofu ran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol.

[0032] In a further embodiment, the compounds of the disclosure are used as medicaments. Accordingly, the disclosure also includes a compound of the disclosure for use as a medicament and in the making or manufacture of a medicament.

[0033] In other embodiments, the compounds of the disclosure are used as ingredients in compositions and pharmaceutical compositions, including medicaments or other compositions and in the making or manufacture of compositions and pharmaceutical compositions.

[0034] The present disclosure also includes a method of treating a disease, disorder, and / or condition comprising administering a therapeutically effective amount of one or more compounds of the disclosure to a subject in need thereof. In some embodiments, medicaments and other compositions for treatment of a disease, disorder, and / or condition are provided that include one or more of the compounds of the disclosure. In some embodiments, the present disclosure relates to use of one or more compounds of this disclosure in the making or manufacture of a medicament or other composition for treating a disease, disorder, and / or condition.

[0035] The present disclosure also includes a method of treating depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout. In some embodiments, the present disclosure also includes medicaments and other compositions for treatment of depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout. In some embodiments, the present disclosure relatesto use of one or more compounds of this disclosure in the making or manufacture of a medicament or other composition for treating depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout.

[0036] The disclosure additionally provides a process for the preparation of compounds of the disclosure and related compositions. The disclosure further provides use of compounds of the disclosure in the making or manufacture of medicines and other compositions. General and specific processes are discussed in more detail below and set forth in the examples below.

[0037] This disclosure further provides intermediates for the compounds disclosed herein, methods of making the intermediates, and methods for making the compounds from the intermediates.

[0038] Other features of the present disclosure will become apparent from the following detailed description. It should be understood, however, that the detailed description and the specific examples, while indicating embodiments of the disclosure, are given by way of illustration only and the scope of the claims should not be limited by these embodiments but should be given the broadest interpretation consistent with the description as a whole.DETAILED DESCRIPTIONDefinitions

[0039] Unless otherwise indicated, the definitions and embodiments described in this and other sections are intended to be applicable to all embodiments and aspects of the present disclosure herein described for which they are suitable as would be understood by a person skilled in the art.

[0040] The present description refers to a number of chemical terms and abbreviations used by those skilled in the art. Nevertheless, definitions of selected terms are provided for clarity and consistency.

[0041] As used in the present disclosure, the singular forms “a,” “an,” and “the” include plural references unless the content clearly dictates otherwise. For example, an embodiment including “a compound" should be understood to present certain aspects with one compound, or two or more additional compounds. It will be understood by those with skill in the art that if a specific number of an introduced claim element is intended, such intent will be explicitly recited in the claim, and in the absence of such recitation no such limitation is present. For a non-limiting example, as an aid to understanding, the appended claims contain usage of the introductory phrases “at least one” and “one or more” to introduce claim elements. However, the use of such phrases should not be construed to imply that the introduction of a claim element by the indefinite articles “a” or “an” limits any particular claim containing such introduced claim element to embodiments containing only one such element, even when the same claim includes the introductory phrase “one or more” or “at least one" and indefinite articles, such as “a” or “an”; the same holds true for the use in the claims of definite articles.

[0042] The terms “about,” “substantially,” and “approximately,” as used herein, mean a reasonable amount of deviation of the modified term such that the end result is not significantly changed. These terms of degree should be construed as including a deviation of at least ±5% of the modified term if this deviation would not negate the meaning of the word it modifies or unless the context suggests otherwise to a person skilled in the art.

[0043] In embodiments comprising an “additional” or “second” component, such as an additional or second compound, the second component, as used herein, is not the same component as the other components or first component. A “third” component is not the same component as the other, first and second components and further enumerated or “additional” components are similarly different components. It should be understood, for example, that although a first group and a second group refer to two groups, the first and second groups may be the same species, for example, both C1-C6alkyl, or methyl. “First,” “second,” “third,” etc. in this context is not meant to imply an order or sequence, other than the order in which the terms appear in the claims, unless the claims clearly indicate otherwise.

[0044] The term “administered," as used herein, means administration of a therapeutically effective amount of one or more compounds or compositions of the disclosure to a cell, tissue, organ, or subject.

[0045] The term “alkyl,” as used herein, whether it is used alone or as part of another group, means substituted or unsubstituted, straight or branched chain, saturated hydrocarbon groups, unless the context clearly indicates otherwise, e.g., an “unsubstituted alkyl” is not substituted. The number of carbon atoms that are possible in the referenced alkyl group are indicated by the prefix “Cn-Cm” and “Co,” where n, m, and o are integers. Thus, for example, the term “C1-C6alkyl" (or “C1- salkyl”) means an alkyl group having 1 , 2, 3, 4, 5, or 6 carbon atoms and includes, for example, any of the hexyl alkyl and pentyl alkyl isomers as well as n-, iso-, sec- and tert-butyl, n- and isopropyl, ethyl, and methyl. As another example, “C1-C4alkyl” refers to n-, iso-, sec- and tert-butyl, n- and isopropyl, ethyl, and methyl. Unless otherwise stated, an “alkyl” group includes all isomers. As another example, “C1alkyl” refers to a methyl group; “C2alkyl” refers to an ethyl group; “C3alkyl” refers to a propyl group (e.g., n-propyl or iso-propyl)); “C4alkyl” refers to a butyl group (e.g., n- butyl, sec-butyl, isobutyl, or tert-butyl); "C5alkyl" refers to a pentyl group and any of its isomers; and "C6alkyl” refers to a hexyl group and any of its isomers. As another example, “propyl” includes n-propyl and iso-propyl; “butyl” includes n-butyl, sec-butyl, isobutyl, and tert-butyl; etc.

[0046] The term “alternate isotope thereof and “alternative isotope thereof as used herein, refers to an isotope of an element that is other than the isotope that is most abundant in nature.

[0047] The term “and / or,” as used herein, means that one or more of the listed items are present, or used, individually or in combination. In effect, this term means that “at least one of or “one or more” of the listed items is used or present. The term “and / or” with respect to pharmaceutically acceptable salts and / or solvates thereof means that the compounds of the disclosure exist as individual salts or solvates, as well as a combination of, for example, a salt of a solvate of a compound of the disclosure. As used herein, the term “and / or” means either or both (or any combination or all of the terms or expressions referred to), e.g., “A, B, and / or C” encompasses A alone; B alone; C alone; A and B; A and C; B and C; and A, B, and C.

[0048] The term "any member, combination, or subset thereof,” as used herein, when used to refer to a preceding list of possible members, means that any individual listed member, possible combination of listed members, or subset of listed members may be included. For example, if Z is selected from A, B, C, and D, including any member, combination, or subset thereof, then Z may be A, B, C, and D; A, B, and C; A, B, and D; A, C, and D; B, C, and D; A and B; A and C; A and D; B and C; B and D; C and D; A alone; B alone; C alone; or D alone.

[0049] The term “aryl,” as used herein, whether it is used alone or as part of another group, refers to a substituted or unsubstituted aromatic carbocyclic ring or multi-ring structures (e.g., bicyclic). For example, for an aryl group that contains the prefix C6-C10, the corresponding carbocyclic group(s) contains 6, 7, 8, 9, or 10 carbon ring atoms.

[0050] The term “available," as in “available hydrogen atoms" or “available atoms,” refers to atoms that would be known to a person skilled in the art to be capable of replacement by a substituent.

[0051] The term “benzofused,” as used herein, refers to a polycyclic group in which a benzene ring is fused with another ring.

[0052] The term “carbocyclic group,” as used herein, refers to substituted or unsubstituted cyclic groups where all ring members are carbon atoms.

[0053] The term “composition(s) of the disclosure” or “composition(s) of the present disclosure” and the like, as used herein, refers to a composition, such a pharmaceutical composition, comprising one or more compounds of the disclosure.

[0054] The term “compound(s) of the disclosure” or “compound(s) of the present disclosure” and the like, as used herein, refers to a compound Formula (I) and includes, in some embodiments, pharmaceutically acceptable salts, solvates, and / or prodrugs thereof.

[0055] As used in this disclosure and claim(s), the words “comprising” (and any form of comprising, such as “comprise” and “comprises”), “having” (and any form of having, such as “have” and “has”), “including” (and any form of including, such as “include” and “includes”) or “containing” (and any form of containing, such as “contain” and “contains”), are inclusive or open- ended and do not exclude additional, unrecited elements or process steps.

[0056] The term “consisting" and its derivatives, as used herein, are intended to be closed terms that specify the presence of the stated features, elements, components, groups, integers and / or steps and also exclude the presence of other unstated features, elements, components, groups, integers, and / or steps.

[0057] The term “consisting essentially of,” as used herein, is intended to specify the presence of the stated features, elements, components, groups, integers, and / or steps as well as those thatdo not materially affect the basic and novel characteristic(s) of those features, elements, components, groups, integers, and / or steps.

[0058] All “cyclic” groups, including aryl, heteroaryl, heterocycloalkyl, and cycloalkyl groups, contain one ring or more than one ring (i.e., are optionally polycyclic), unless otherwise indicated. When a cyclic group contains more than one ring, the rings may be fused, bridged, spirofused, or linked by a bond.

[0059] The term “cycloalky I,” as used herein, whether it is used alone or as part of another group, means a substituted or unsubstituted, saturated or unsaturated non-aromatic, carbocyclic ring or multi-ring structures (e.g., bi-cyclic), unless otherwise specified. The term C3-C7cycloalkyl (or C3-7cycloalkyl) means a cycloalkyl group having 3, 4, 5, 6, or 7 ring carbon atoms. A cycloalkyl is optionally fused to another ring, including fused to an aryl ring (e.g., benzofused) or heteroaryl ring.

[0060] The term “disease, disorder, or condition,” as used herein, refers to a disease, disorder, or condition treated or treatable using one or more compounds of the disclosure herein described.

[0061] As used herein, the term “effective amount” or “therapeutically effective amount” means an amount of one or more compounds of the disclosure that is effective, at dosages and for periods of time necessary to achieve the desired result. For example, in the context of treating a disease, disorder, or condition, an effective amount is an amount that, for example, treats, palliates, and / or prevents said disease, disorder, or condition compared to the non-treatment, non-palliation, or non-prevention without administration of the one or more compounds.

[0062] The suffix “ene” at the end of a group (for example “alkylene”) means that the group is bivalent, that is that it is bonded to two variables each on a different end of or location on the group. An alkylene may be substituted or unsubstituted, straight or branched chain. The number of carbon atoms that are possible in the referenced alkylene group are indicated by the prefix “Cn. Cm" and “Co” where n, m, and o are integers. Thus, for example, the term “C1-C6alkylene” (or “C1-6alkylene”) means an alkylene group having 1, 2, 3, 4, 5, or 6 carbon atoms and includes, for example, any of the hexylene and pentylene isomers as well as n-, iso-, sec-, and tert-butylene, n- and iso-propylene, ethylene, and methylene. Unless otherwise stated, an “alkylene” group includes all isomers. As another example, “C1alkylene” refers to a methylene group; “C2alkylene” refers to an ethylene group; "C3alkylene" refers to a propylene group (e.g., n-propylene or isopropylene)); “C4alkylene” refers to a butylene group (e.g., n-butylene, sec-butylene, isobutylene,or tert-butylene); “C5alkylene” refers to a pentylene group and any of its isomers; and “C6alkylene” refers to a hexylene group and any of its isomers. As another example, “propylene” includes n- propylene and iso-propylene; “butylene" includes n-butylene, sec-butylene, isobutylene, and tertbutylene)); etc.

[0063] The word “exemplary” is used herein to mean “serving as an example, instance, or illustration.” Any implementation described herein as “exemplary” is not necessarily to be construed as preferred or advantageous over other implementations. Reference throughout this specification to “a select embodiment,” “one embodiment,” “an exemplary embodiment,” “exemplary embodiments,” “an embodiment,” or “embodiments” means that a particular feature, structure, or characteristic described in connection with the embodiment(s) is included in at least one embodiment. Thus, appearances of the phrases “in a select embodiment,” “in one embodiment," "in an exemplary embodiment,” "in exemplary embodiments,” "in some embodiments,” “in an embodiment,” or “in embodiments” in various places throughout this specification are not necessarily referring to the same embodiment(s) or only a single embodiment. The embodiments may be, for example, combined with one another in various combinations and modified to include features of one another.

[0064] A first ring being “fused” with a second ring means the first ring and the second ring share two adjacent atoms there between.

[0065] The term “halogen” (or “halo”) whether it is used alone or as part of another group, refers to a halogen atom and includes fluoro, chloro, bromo, and iodo.

[0066] The term “heteroaryl,” as used herein, whether it is used alone or as part of another group, refers to substituted or unsubstituted aromatic ring or multi-ring structures (e.g., bi-cyclic), in which one or more of the atoms of the aromatic ring are a heteromoiety independently selected from O, S, and N, including oxidized or substituted versions thereof (e.g., S(O) and S(O)2), and the remaining atoms are C, unless otherwise specified. When a heteroaryl group contains the prefix of, for example, C5-C10, this prefix indicates that the corresponding carbocyclic group(s) contains 5, 6, 7, 8, 9, or 10 carbon atoms in the ring, in which one or more, suitably 1 to 5, of the ring atoms is replaced with a heteroatom as defined above. Heteroaryl groups may also be preceded by, for example, “5- to 10-membered” which refers to the total number of ring atoms (in this example, 5, 6, 7, 8, 9, or 10 atoms) in the aromatic ring or multi-ring structures, including the heteroatom(s). Heteroaryl groups may be benzofused.

[0067] The term “heterocycloalkyl,” as used herein, whether it is used alone or as part of another group, refers to substituted or unsubstituted, saturated or non-saturated, non-aromatic ring or multi-ring structures (e.g., bi-cyclic), in which one or more of the ring atoms of the non- aromatic ring or multi-ring structure are independently selected from O, S, and N, including oxidized or substituted versions thereof (e.g., S(O) and S(O)2), and the remaining atoms are C, unless otherwise specified. Heterocycloalkyl groups are either saturated or unsaturated (i.e., contain one or more double bonds) and / or optionally comprise one or more C=O groups (i.e., one or more carbon atoms in the ring is oxidized to C=O). When a heterocycloalkyl group contains a prefix, such as C3-C10, this prefix indicates that the corresponding carbocyclic group contains 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms in the ring, in which one or more, suitably 1 to 5, of the ring atoms are replaced with a heteromoiety independently selected from O, S, and N including oxidized or substituted versions thereof, and the remaining atoms are C. Similarly, heterocycloalkyl groups may also be preceded by a prefix, such as “3- to 10-membered,” which refers to the total number of atoms in the ring(s) (in this example, 3, 4, 5, 6, 7, 8, 9, or 10 atoms). Heterocycloalkyl groups are optionally fused to another ring, including fused to an aryl ring (e.g., benzofused) or heteroaryl ring.

[0068] As used herein, the term “one or more” item includes a single item selected from the list as well as two or more items (e.g., combinations and mixtures) selected from the list.

[0069] The term “one or more available atoms are optionally and independently replaced with one or more respective alternative isotopes thereof,” and the like, as used herein, means that at least one available atom, optionally a plurality, and optionally each and every available atom, is optionally and independently replaced with an isotope of that atom having the same atomic number, but an atomic mass or mass number different from the atomic mass or mass number predominantly found in nature. When a compound comprises an atom that has been replaced with an alternative isotope thereof, the compound comprises that alternative isotope in greater amounts than would otherwise be present in the compound if said replacement had not taken place. In some embodiments, the alternative isotope is deuterium.

[0070] The term “one or more available hydrogen atoms are optionally and independently replaced with one or more respective deuterium atoms," and the like, as used herein, means that at least one available hydrogen atom, optionally a plurality, and optionally each and every available hydrogen atom, is optionally and independently replaced with a deuterium atom. When a compound comprises a hydrogen atom that has been replaced with a deuterium atom, thecompound comprises that deuterium atom in greater amounts than would otherwise be present in the compound if said replacement had not taken place.

[0071] The term “one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms,” and the like, as used herein, means that at least one available hydrogen atom, optionally a plurality, and optionally each and every available hydrogen atom, is optionally and independently replaced with a specified halogen atom (e.g., a fluorine atom, a chlorine atom, and / or a bromine atom), and the replacements are independent of one another, e.g., the compound may include only F; only Cl; only Br; both F and Cl; both F and Br; both Cl and Br; or a combination of F, Cl, and Br replacements.

[0072] The term “one or more available hydrogen atoms are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms,” and the like, as used herein, means that at least one available hydrogen atom, optionally a plurality, and optionally each and every available hydrogen atom of the specified member(s) or group, is optionally and independently replaced with a specified halogen atom (e.g., a fluorine atom, a chlorine atom, and / or a bromine atom), and the replacements are independent of one another, e.g., the replacements may include only F, only Cl, only Br, both F and Cl, both F and Br, both Cl and Br, or a combination of F, Cl, and Br replacements.

[0073] The term “optionally substituted," as used herein, means that the subject group is unsubstituted or substituted and the terms “optionally substituted” and “unsubstituted or substituted” are used interchangeably herein. As used herein, when referring to more than one item or “each” item, “optionally substituted” and “unsubstituted or substituted” means that the items are independently unsubstituted or substituted with respect to one another, e.g., for item A and item B, both may be substituted, both may be unsubstituted, or one may be substituted and the other unsubstituted. Additionally, as used herein, the term ‘optionally substituted” when referring to more than one item means that if more than one of the items is substituted, the substitutions may be independent from one another, e.g., for item A and item B that are both substituted, item A may have a first substitution and item B may have a second substitution that is the same or different from the first substitution of item A.

[0074] “Palliating” a disease, disorder, or condition means that the extent and / or undesirable clinical manifestations of a disease, disorder, or condition are lessened and / or time course of the progression is slowed or lengthened, as compared to not treating the disorder.

[0075] The term “pharmaceutically acceptable” means compatible with the treatment of subjects.

[0076] The term ‘pharmaceutically acceptable carrier'’ means a non-toxic solvent, dispersant, excipient, adjuvant, or other material which is mixed or otherwise combined with the active ingredient in order to permit the formation of a pharmaceutical composition, i.e., a dosage form capable of administration to a subject.

[0077] The term “pharmaceutically acceptable salt” means either an acid addition salt or a base addition salt which is suitable for, or compatible with, the treatment of subjects. An acid addition salt suitable for, or compatible with, the treatment of subjects is any non-toxic organic or inorganic acid addition salt of any basic compound. A base addition salt suitable for, or compatible with, the treatment of subjects is any non-toxic organic or inorganic base addition salt of any acidic compound.

[0078] The term “prevention” or “prophylaxis,” or synonym thereto, as used herein, refers to a reduction in the risk or probability of a patient becoming afflicted with a disease, disorder, or condition or manifesting a symptom associated with a disease, disorder, or condition.

[0079] The term “prodrug,” as used herein, means a compound, or salt of a compound, that, after administration, is converted into an active drug.

[0080] The term “protecting group” or “PG” and the like, as used herein, refers to a chemical moiety which protects or masks a reactive portion of a molecule to prevent side reactions in those reactive portions of the molecule, while manipulating or reacting a different portion of the molecule. After the manipulation or reaction is complete, the protecting group is removed under conditions that do not degrade or decompose the remaining portions of the molecule. The selection of a suitable protecting group can be made by a person skilled in the art. Many conventional protecting groups are known in the art, for example as described in “Protective Groups in Organic Chemistry,” McOmie, J.F.W. Ed., Plenum Press, 1973, in Greene, T.W. and Wuts, P.G.M., “Protective Groups in Organic Synthesis,” John Wiley & Sons, 3rdEdition, 1999 and in Kocienski, P. Protecting Groups, 3rd Edition, 2003, Georg Thieme Verlag (The Americas).

[0081] The term “solvate,” as used herein, means a compound, or a salt or prodrug of a compound, wherein molecules of a suitable solvent are incorporated in the crystal lattice. A suitable solvent is physiologically tolerable at the dosage administered.

[0082] The term “subject,” as used herein, includes all members of the animal kingdom including mammals, and suitably refers to humans. Thus, the methods of the present disclosure are applicable to both human therapy and veterinary applications.

[0083] The term “substituted,” as used herein, means, unless otherwise indicated, that the referenced group is substituted with one or more independently selected substituents. When a group is substituted with more than one substituent selected from a list of substituents, each of the substituents is independently selected from the listed group of substituents unless otherwise indicated.

[0084] The term “suitable,” as used herein, means that the selection of the particular compound or conditions would depend on the specific synthetic manipulation to be performed, the identity of the molecule(s) to be transformed and / or the specific use for the compound, but the selection would be well within the skill of a person trained in the art. All process / method steps described herein are to be conducted under conditions sufficient to provide the product shown. A person skilled in the art would understand that all reaction conditions, including, for example, reaction solvent, reaction time, reaction temperature, reaction pressure, reactant ratio, and whether or not the reaction should be performed under an anhydrous or inert atmosphere, can be varied to control the yield of the desired product and it is within their skill to do so.

[0085] The term “therapeutic agent,” as used herein, refers to any drug or active agent that has a pharmacological effect when administered to a subject.

[0086] The term “treating” or “treatment,” as used herein, and as is well understood in the art, means an approach for obtaining beneficial or desired results, including clinical results. Beneficial or desired clinical results include, but are not limited to, alleviation or amelioration of one or more symptoms or conditions, diminishment of extent of disease, stabilized (i.e„ not worsening) state of disease, preventing spread of disease, delay, or slowing of disease progression, amelioration or palliation of the disease state, diminishment of the reoccurrence of disease and remission (whether partial or total), whether detectable or undetectable. "Treating” and "treatment” can also mean prolonging survival as compared to expected survival if not receiving treatment. “Treating” and “treatment,” as used herein, also include prophylactic treatment. Treatment methodscomprise administering to a subject a therapeutically effective amount of one or more of the compounds of the disclosure and optionally consist of a single administration, or alternatively comprise a series of administrations.

[0087] The term “treating a disease, disorder, or condition,” as used herein, means that the disease, disorder, or condition to be treated is affected by, modulated by, and / or has some biological basis.II. Compounds

[0088] The present disclosure includes a compound of Formula (I):or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, Q, X, m, n, o, and p are as defined (and provisos and exclusions provided for) in the Summary above and exemplified below.

[0089] In some embodiments, the compound of Formula (I) is not selected from the following, and in some embodiments the compound of Formula (I) is not selected from a partially or fully deuterated analog, and in some embodiments the compound of Formula (I) is not selected from a partially or fully halogenated analog, and in some embodiments the compound of Formula (I) is not selected from a partially or fully deuterated and halogenated analog of the following:4-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1H-inden-1-yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1 λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzothiophene-1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1 -methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol.

[0090] In some embodiments, X is CR18R19. In some embodiments, X is O. In some embodiments, X is S. In some embodiments, X is S(O). In some embodiments, X is S(O)2. In some embodiments, X is selected from CR18R19, O, S, S(O), and S(O)2, including any member, combination, or subset thereof.

[0091] In some embodiments, R1is selected from H, D, and halo. In some embodiments, R1is selected from optionally substituted C1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1- C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof.

[0092] In some embodiments, R1is selected from unsubstituted C1-C6alkyl, unsubstituted C3- C6cycloalkyl, unsubstituted OC1-C6alkyl, unsubstituted SC1-C6alkyl, unsubstituted OC1- C6alkyleneC(O)OH, and unsubstituted OC1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R1is selected from substituted C1-C6alkyl, substituted C3-C6cycloalkyl, substituted OC1-C6alkyl, substituted SC1-C6alkyl, substituted OC1- C6alkyleneC(O)OH, and substituted OC1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof.

[0093] In some embodiments, R1is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3- C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof.

[0094] I n some embodiments, R1is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R1is D. In some embodiments, R1is OCH3. In someembodiments, R1is selected from propyl,In some embodiments, R1is selected from

[0095] In some embodiments, R2is selected from H, D, and halo. In some embodiments, R2is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R2is D. In some embodiments, R3is selected from F, Cl, Br, and I, including any member, combination, or subset thereof.

[0096] In some embodiments, R2is selected from optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1- C6alkyleneOC1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC3- C6cycloalkyl, optionally substituted OC1-C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6- membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl, including any member, combination, or subset thereof.

[0097] In some embodiments, R2is selected from unsubstituted C1-C6alkyl, unsubstituted OC1- C6alkyl, unsubstituted SC1-C6alkyl, unsubstituted OC1-C6alkyleneOC1-C6alkyl, unsubstituted C3. C6cycloalkyl, unsubstituted OC3-C6cycloalkyl, unsubstituted OC1-C6alkyleneC3-C6cycloalkyl, unsubstituted 5- to 6-membered heterocycloalkyl, unsubstituted O(5- to 6-membered) heterocycloalkyl, unsubstituted C6aryl, unsubstituted C1-C6alkyleneC6aryl, unsubstituted 5- to 6- membered heteroaryl, unsubstituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and unsubstituted C1-C6alkylene(5- to 6-membered) heteroaryl, including any member, combination, or subset thereof.

[0098] In some embodiments, R2is selected from substituted C1-C6alkyl, substituted OC1- C6alkyl, substituted SC1-C6alkyl, substituted OC1-C6alkyleneOC1-C6alkyl, substituted C3- C6cycloalkyl, substituted OC3-C6cycloalkyl, substituted OC1-C6alkyleneC3-C6cycloalkyl, substituted 5- to 6-membered heterocycloalkyl, substituted O(5- to 6-membered) heterocycloalkyl, substituted C6aryl, substituted C1-C6alkyleneC6aryl, substituted 5- to 6-membered heteroaryl, substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and substituted C1-C6alkylene(5- to 6-membered) heteroaryl, including any member, combination, or subset thereof. In some embodiments, R2is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof.

[0099] In some embodiments, R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, and optionally substituted OC1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R2is selected from H, D, F, isopropyl, OCH3, and O-propyl, including any member, combination, or subset thereof, wherein one or more available hydrogen atoms of R2are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R2is selected from unsubstituted C3- C6cycloalkyl, unsubstituted OC3-C6cycloalkyl, and unsubstituted OC1-C6alkyleneC3-C6cycloalkyl, including any member, combination, or subset thereof. In some embodiments, R2is selected from substituted C3-C6cycloalkyl, substituted OC3-C6cycloalkyl, and substituted OC1-C6alkyleneC3-C6cycloalkyl, including any member, combination, or subset thereof. In some embodiments, R2is selected from C3-C6cycloalkyl, OC3-C6cycloalkyl, and OC1-C6alkyleneC3-C6cycloalkyl, including any member, combination, or subset thereof, wherein R2is substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and 0C1-C4alkyl, including any member, combination, or subset thereof.

[0100] In some embodiments, R2comprises a heterocycloalkyl moiety and is selected from optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6- membered) heterocycloalkyl, and optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, including any member, combination, or subset thereof. In some embodiments, the heterocycloalkyl moiety and / or the alkylene moiety of R2is unsubstituted. In some embodiments, the heterocycloalkyl moiety and / or the alkylene moiety of R2is independently substituted. In some embodiments, the heterocycloalkyl moiety and / or the alkylene moiety of R2is substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1- C4alkyl, and OC1-C4alkyl, including any member, combination, or subset thereof. In some embodiments, the heterocycloalkyl moiety of R2comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, wherein the heterocycloalkyl moiety of R2optionally and additionally comprises one or two C=O groups.

[0101] In some embodiments, R2comprises an aryl moiety and is selected from optionally substituted C6aryl (or phenyl) and optionally substituted C1-C6alkyleneC6aryl (e.g., benzyl). In some embodiments, the aryl moiety of R2is unsubstituted. In some embodiments, the aryl moiety of R2is independently substituted with one or more substituents. In some embodiments, the aryl moiety of R2is independently substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and OC1-C4alkyl, including any member, combination, or subset thereof.

[0102] In some embodiments, R2comprises a heteroaryl moiety and is selected from optionally substituted 5- to 6-membered heteroaryl and optionally substituted C1-C6alkylene(5- to 6- membered) heteroaryl. In some embodiments, the heteroaryl moiety of R2is unsubstituted. In some embodiments, the heteroaryl moiety of R2is independently substituted with one or more substituents. In some embodiments, the heteroaryl moiety of R2is substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and OC1-C4alkyl, including any member, combination, or subset thereof. In some embodiments, the heteroaryl moiety of R2comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, and the heteroaryl moiety optionally and additionally comprises one or two C=O groups.

[0103] In some embodiments, R2is or comprises a member selected from:including any member, combination, or subset thereof.

[0104] In some embodiments, R2and R3are linked to one another to form an optionally substituted 3- to 5-membered heterocycloalkyl. In some embodiments, R2and R3are linked to one another to form an optionally substituted 5-membered heterocycloalkyl. In some embodiments, R2and R3are linked to one another with O-(CH2)1-2-O-, and in some embodimentswith -O-CH2-O-. In some embodiments, R2and R3are linked to one another to form an unsubstituted heterocycloalkyl. In some embodiments, R2and R3are linked to one another to form a substituted heterocycloalkyl. In some embodiments, the heterocycloalkyl comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, wherein the at least one heterocycloalkyl optionally and additionally comprises one or two C=O groups. In some embodiments, the heterocycloalkyl comprises 2 oxygen ring atoms.

[0105] In some embodiments, R3is selected from H, D, and halo. In some embodiments, R3is selected from substituted C1-C6alkyl and substituted OC1-C6alkyl. In some embodiments, C1- C6alkyl and OC1-C6alkyl of R3is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R3is selected from unsubstituted C1-C6alkyl and unsubstituted OC1-C6alkyl. In some embodiments, R3is selected from H, OCH3, and O-propyl, wherein one or more available hydrogen atoms of R3are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R3is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R3is D. In some embodiments, R3is F.

[0106] In some embodiments, R4is selected from H, D, and halo. In some embodiments, R4is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R4is D. In some embodiments, R4is selected from F, Cl, Br, and I, including any member, combination, or subset thereof. In some embodiments, R4is F.

[0107] In some embodiments, R4is selected from substituted C1-C6alkyl and substituted OC1- C6alkyl. In some embodiments, R4is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3- C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R4is selected from unsubstituted C1-C6alkyl and unsubstituted OC1-C6alkyl. In some embodiments, R4is selected from H and OCH3, wherein one or more available hydrogen atoms of R4are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0108] In some embodiments, R5is selected from H, D, halo, and optionally substituted C1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, R5isselected from H, D, and optionally substituted C1-C6alkyl. In some embodiments, R5is selected from halo and optionally substituted C1-C6alkyl. In some embodiments, R5is selected from H, D, and halo. In some embodiments, R5is substituted C1-C6alkyl. In some embodiments, R5is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R5is unsubstituted C1-C6alkyl. In some embodiments, R5is selected from H and CH3, wherein one or more available hydrogen atoms of R5are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R5is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R5is D. In some embodiments, R5is F.

[0109] In some embodiments, R6is selected from H, D, halo, and optionally substituted C1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, R6is selected from H, D, and optionally substituted C1-C6alkyl. In some embodiments, R6is selected from halo and optionally substituted C1-C6alkyl. In some embodiments, R6is selected from H, D, and halo. In some embodiments, R6is substituted C1-C6alkyl. In some embodiments, R6is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C6-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R6is unsubstituted C1-C6alkyl. In some embodiments, R6is selected from H and CH3, wherein one or more available hydrogen atoms of R6are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R6is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R6is D. In some embodiments, R6is F.

[0110] In some embodiments, R7is selected from H, D, halo, and OH, and optionally substituted C1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R7is substituted C1-C6alkyl. In some embodiments, R7is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R7is unsubstituted C1-C6alkyl. In some embodiments, R7is selected from H and CH3, wherein one ormore available hydrogen atoms of R7are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R7is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R7is D. In some embodiments, R7is F.

[0111] In some embodiments, Q is selected as Q1 to provide a compound having the structure:wherein R1, R2, R3, R4, R5, R8, R7, R8, R9, R18, R19, X, and m are as defined (and provisos and exclusions provided for) herein.

[0112] In some embodiments, “m” is an integer, and in some embodiments, “m" is 0, 1 , or 2. In some embodiments, “m” is 0. In some embodiments, “m” is 1, 2, or selected from 1 and 2.

[0113] In some embodiments, each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R8is independently halo. In some embodiments, each R8is F. In some embodiments, each R8is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, one or more R8is independently substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, each R8is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl,including any member, combination, or subset thereof. In some embodiments, each R8is independently CH3, wherein one or more available hydrogen atoms of R8are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R8is independently selected from OC1-C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R8are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R8is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F, including any member, combination, or subset thereof.

[0114] In some embodiments, R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R9is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R9is D. In some embodiments, R9is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R9is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1- C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R9is selected from unsubstituted C1- C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R9is selected from H and CH3. In some embodiments, R9is selected from H, D, CH3, CD3, and CF3, including any member, combination, or subset thereof. In some embodiments, R9is substituted CH2CH2OCH3. In some embodiments, R9is unsubstituted CH2CH2OCH3.

[0115] In some embodiments, Q is selected as Q2 to provide a compound having a structure:wherein R1, R2, R3, R4, R5, R6, R7, R10, R11, R18, R19, X, and n are as defined (and provisos and exclusions provided for) herein.

[0116] In some embodiments, “n” is an integer. In some embodiments, “n” is selected from 0, 1, and 2. In some embodiments, “n” is 0. In some embodiments, “n” is 1 , 2, or selected from 1 and 2.

[0117] In some embodiments, each R10is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R10is independently halo, and in some embodiments each R10is F. In some embodiments, each R10is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, one or more R10is independently substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, each R10is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R10is independently CH3, wherein one or more available hydrogen atoms of R10are optionally andindependently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R10is independently selected from OC1-C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R10are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R10is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F, including any member, combination, or subset thereof.

[0118] In some embodiments, R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R11is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R11is D. In some embodiments, R11is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R11is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1- CaalkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R11is selected from unsubstituted C1- C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R11is selected from H and CH3. In some embodiments, R11is selected from H, D, CH3, CD3, and CF3, including any member, combination, or subset thereof. In some embodiments, R11is C1-C6alkyleneOC1-C6alkyl, wherein one or more available hydrogen atoms of R11are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R11is substituted CH2CH2OCH3. In some embodiments, R11is unsubstituted CH2CH2OCH3.

[0119] In some embodiments, Q is selected as Q3 to provide a compound having a structure:wherein R1, R2, R3, R4, R5, R6, R7, R12, R13, R18, R19, X, and o are as defined (and provisos and exclusions provided for) herein.

[0120] In some embodiments, “o” is an integer. In some embodiments, “o” is 0, 1 , or 2. In some embodiments, “o” is 0. In some embodiments, “o” is 1 , 2, or selected from 1 and 2.

[0121] In some embodiments, each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R12is independently halo. In some embodiments, each R12is F. In some embodiments, each R12is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, one or more R12are independently substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, each R12is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R12is independently CH3, wherein one or more available hydrogen atoms of R12are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R12is independently selected from OC1-C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R12are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respectivedeuterium atoms. In some embodiments, each R12is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F, including any member, combination, or subset thereof.

[0122] In some embodiments, R13is selected from H, optionally substituted C1-C6alkyl, and optionally substituted C1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R13is H not replaced with a halogen atom or an alternative isotope thereof. In some embodiments, R13is D. In some embodiments, R13is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R13is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1- C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R13is selected from unsubstituted C1- C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R13is selected from H and CH3. In some embodiments, R13is selected from H, D, CH3, CD3, and CF3, including any member, combination, or subset thereof. In some embodiments, R13is C1-C6alkyleneOC1-C6alkyl, wherein one or more available hydrogen atoms of R13are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R13is substituted CH2CH2OCH3. In some embodiments, R13is unsubstituted CH2CH2OCH3.

[0123] In some embodiments, Q is selected as Q4 to provide a compound having a structure:wherein R1, R2, R3, R4, R5, R6, R7, R14, R15, R16, R17, R18, R19, X, and p are as defined (and provisos and exclusions provided for) herein.

[0124] In some embodiments, “p” is an integer. In some embodiments, “p” is 0, 1, or selected from 1 and 2. In some embodiments, “p” is 0. In some embodiments, “p” is 1 or 2.

[0125] In some embodiments, each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R14is independently halo. In some embodiments, each R14is F. In some embodiments, each R14is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1- C6alkyl, including any member, combination, or subset thereof. In some embodiments, one or more R14are independently substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, each R14is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, each R14is independently CH3, wherein one or more available hydrogen atoms of R14are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R14is independently selected from OC1-C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R14are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, each R14is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F, including any member, combination, or subset thereof.

[0126] In some embodiments, R15is selected from H, optionally substituted C1-C6alkyl, and optionally substituted C1-C6alkyleneOC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R15is H not replaced with a halogen or an alternative isotope thereof. In some embodiments, R15is D. In some embodiments, R15is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R15is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1- C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R15is selected from unsubstituted C1-C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl. In some embodiments, R15is selected from H and CH3. In some embodiments, R15is selected from H, D, CH3, CD3, and CF3, including any member, combination, or subset thereof. In some embodiments, R15is C1-C6alkyleneOC1-C6alkyl, wherein one or more available hydrogen atoms of R15are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R15is substituted CH2CH2OCH3. In some embodiments, R15is unsubstituted CH2CH2OCH3.

[0127] In some embodiments, R16and R17are included in a structurein which R16is selected from H, halo, OH, and optionally substituted C1-C6alkyl, including any member, combination, or subset thereof, and R17is selected from H, halo, OH, and optionally substituted C1-C6alkyl, including any member, combination, or subset thereof.

[0128] In some embodiments, R16is selected from H, halo, and OH, including any member, combination, or subset thereof. In some embodiments, R16is substituted C1-C6alkyl. In some embodiments, R16is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10- membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R16is unsubstituted C1-C6alkyl. In some embodiments, R16is independently selected from H, OH, F and CH3, wherein one or more available hydrogen atoms of R16are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R16is H not replaced with a halogen atom or an alternative substitute thereof. In some embodiments, R16is D. In some embodiments, R16is F.

[0129] In some embodiments, R17is selected from H, halo, and OH, including any member, combination, or subset thereof. In some embodiments, R17is substituted C1-C6alkyl. In some embodiments, R17is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10- membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R17is unsubstituted C1-C6alkyl. In some embodiments, R17is independently selected from H, OH, F and CHs, wherein one or more available hydrogen atoms of R17are optionally and independently replaced with one or morerespective fluorine atoms and / or one or more respective deuterium atoms. In some embodiments, R17is H not replaced with a halogen atom or an alternative substitute thereof. In some embodiments, R17is D. In some embodiments, R17is F.

[0130] In some embodiments,is replaced within which R16and R17on the same carbon atom are taken together with the bonded carbon atom to form a carbonyl group.

[0131] In some embodiments, X is CR18R19, wherein R18is selected from H, halo, optionally substituted C1-C6alkyl, optionally substituted C1-C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof, and wherein R19is selected from H, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof.

[0132] In some embodiments, R18and R19are each H not replaced by a halogen atom or an alternative isotope thereof. In some embodiments, R18and R19are each D. In some embodiments, R18and R19are each halo. In some embodiments, R18and R19are each F.

[0133] In some embodiments, R18is selected from H and halo. In some embodiments, R18is H not replaced by a halogen atom or an alternative isotope thereof. In some embodiments, R18is D. In some embodiments, R18is halo. In some embodiments, R18is F. In some embodiments, R18is selected from substituted C1-C6alkyl, substituted C1-C6alkyleneOC1-C6alkyl, and substituted C1- C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R18is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10- membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R18is selected from unsubstituted C1-C6alkyl, unsubstituted C1-C6alkyleneOC1-C6alkyl, and unsubstituted C1- C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof.

[0134] In some embodiments, R19is selected from H and halo. In some embodiments, R19is H not replaced by a halogen atom or an alternative isotope thereof. In some embodiments, R19is D. In some embodiments, R19is halo. In some embodiments, R19is F. In some embodiments, R19is selected from substituted C1-C6alkyl, substituted C1-C6alkyleneOC1-C6alkyl, and substituted C1-C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, R19is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10- membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl, including any member, combination, or subset thereof. In some embodiments, R18is selected from unsubstituted C1-C6alkyl, unsubstituted C1-C6alkyleneOC1-C6alkyl, and unsubstituted C1- C6alkyleneNHC1-C6alkyl, including any member, combination, or subset thereof.

[0135] In some embodiments, when X is selected from CR18R19, O, and S, then R7is selected from H, halo, and C1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, when X is CR18R19, R18is H, and R19is H, then R7is selected from H, halo, and C1-C6alkyl, including any member, combination, or subset thereof. In some embodiments, when X is CR18R19, then Q is selected from Q3 and Q4. In some embodiments, when X is CR18R19, R18is H, and R19is H, then Q is selected from Q3 and Q4. In some embodiments, when X is selected from CR18H, then R18is not H. In some embodiments, when X is CR18R19, then neither R18nor R19is H.

[0136] In some embodiments of the compound of Formula (I), one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0137] In some embodiments, when one or more available hydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are independently selected from F, Cl, and Br. In some embodiments, when one or more available hydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are independently selected from F and Br. In some embodiments, when one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are independently selected from F and Cl. In some embodiments, when one or more available hydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are F. In some embodiments, when one or more availablehydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are Cl. In some embodiments, when one or more available hydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are Br. In some embodiments, when one or more available hydrogen atoms in a group are optionally and independently replaced with one or more respective halogen atoms, the one or more respective halogen atoms are I. In some embodiments, none of the available hydrogen atoms are replaced with a halogen atom.

[0138] In some embodiments, one or more available atoms are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, the alternative isotope of hydrogen is deuterium. In some embodiments, no available atoms are optionally and independently replaced with alternative isotope thereof. In some embodiments, none of the available hydrogen atoms are replaced with deuterium.

[0139] In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms and / or one or more available hydrogen atoms are optionally and independently replaced with one or more respective deuterium atoms. In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms independently selected from F, Cl, and I and / or one or more available hydrogen atoms are optionally and independently replaced with deuterium. In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms independently selected from F and I and / or one or more available hydrogen atoms are optionally and independently replaced with deuterium. In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms independently selected from F and Cl and / or one or more available hydrogen atoms are optionally and independently replaced with deuterium. In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective fluorine atoms and / or one or more available hydrogen atoms are optionally replaced with deuterium. In some embodiments, one or more available hydrogen atoms are optionally and independently replaced with one or more respective chlorine atoms and / or one or more available hydrogen atoms are optionally replaced with deuterium.

[0140] In some embodiments, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and / or R19optionally and independently are or comprise an optionally substituted C1- C6alkyl. For example and without limitation, in some embodiments, R1is an optionally substituted C1-C6alkyl. In some embodiments, R1comprises an optionally substituted alkyl group, such as when R1is selected from an optionally substituted OC1-C6alkyl, an optionally substituted SC1- C6alkyl, and an optionally substituted OC1-C6alkyleneOC1-C6alkyl.

[0141] In some embodiments, the alkyl groups (e.g., of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and / or R19) are optionally and independently selected from haloalkyl (e.g., C1-C6fluoroalkyl), deuteroalkyl (e.g., C1-C6deuteroalkyl), and deuterohaloalkyl (e.g., C1-C6deuterofluoroalkyl), including any member, combination, or subset thereof. In some embodiments, the one or more halogen atoms of the alkyl groups are optionally and independently selected from F, Cl, Br, and I. In some embodiments, the one or more halogen atoms of the alkyl groups are optionally and independently selected from F, Cl, and Br. In some embodiments, the one or more halogen atoms of the alkyl groups are optionally and independently selected from F and Cl. In some embodiments, the one or more halogen atoms of the alkyl groups are optionally and independently selected from F and Br. In some embodiments, the one or more halogen atoms of the alkyl groups are independently F. In some embodiments, the one or more halogen atoms of the alkyl groups are independently Cl. In some embodiments, the one or more halogen atoms of the alkyl groups are independently Br. In some embodiments, the one or more halogen atoms of the alkyl groups are independently I. In some embodiments, the alkyl groups optionally and independently do not include a halogen atom. In some embodiments, the alkyl groups optionally and independently do not include an alternative isotope. In some embodiments, the alkyl groups optionally and independently include neither a halogen atom nor an alternative isotope.

[0142] In some embodiments, the alkyl groups are optionally and independently substituted C1- C5alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C1- C4alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C1- C3alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C1- C2alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C2- C6alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C3- C6alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C4- C6alkyl. In some embodiments, the alkyl groups are optionally and independently substituted C5- C6alkyl. In some embodiments, the alkyl groups are optionally and independently substitutedC1alkyl (that is, methyl). In some embodiments, the alkyl groups are optionally and independently substituted C2alkyl (that is, ethyl). In some embodiments, the alkyl groups are optionally and independently substituted C3alkyl (that is, propyl). In some embodiments, the alkyl groups are optionally and independently substituted C4alkyl (that is, butyl). In some embodiments, the alkyl groups are optionally and independently substituted C5alkyl (that is, pentyl). In some embodiments, the alkyl groups are optionally and independently substituted C6alkyl (that is, hexyl).

[0143] In some embodiments, the alkyl groups are optionally and independently selected from any combination of the above. In some embodiments, the alkyl groups are independently substituted. In some embodiments, the above alkyl groups are independently unsubstituted.

[0144] In some embodiments, the alkyl groups are optionally and independently selected from CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)2, C(CH3)3, CH2CH2CH2CH2CH3, CH(CH3)CH2CH2CH3, C(CH3)2CH2CH3, CH2CH(CH3)CH2CH3, CH2C(CH3)3, CH2CH2CH2CH2CH2CH3, CH(CH3)CH2CH2CH2CH3, CH(CH3)CH(CH3)CH2CH3, CH(CH3)CH2CH(CH3)2, CH(CH3)C(CH3)3, C(CH3)2CH2CH2CH3, C(CH3)2CH(CH3)2, C(CH3)2C(CH3)3, CH2CH(CH3)CH2CH2CH3, CH2CH(CH3)CH(CH3)2, CH2C(CH3)2CH2CH3, CH2CH2CH(CH3)CH2CH3, CH2CH2C(CH3)3, CH2CH2CH2CH(CH3)2, including any member, combination, or subset thereof.

[0145] In some embodiments, the alkyl groups are optionally and independently selected from CH3, CD2H, CDH2, CD3, CY2H, CYH2, CY3, CH2CH3, CH2CH2Y, CH2CY2H, CH2CY3, CY2CY3, CH2CH2D, CH2CD2H, CH2CD3, CD2CD3, CH2CH2CH3, CH2CH2CHY2, CH2CH2CYH2, CH2CH2CY3, CH2CH2CHD2, CH2CH2CDH2, CH2CH2CD3CH(CH3)2, CH(CY3)2, CH(CHY2)2, CH(CYH2)2, CH(CD3)2, CH(CHD2)2, CH(CDH2)2, C(CH3)3, C(CY3)3, C(CHY2)3, C(CYH2)3, C(CD3)3, C(CHD2)3, C(CDH2)3, CH2CH2CH2CH3, CH2CH2CH2CY3, CH2CH2CH2CD3, CH2CH(CH3)2, CH2CH(CD3)2, CH2CH(CY3)2, CH(CH3)CH2CH3, CH(CH3)CH2CY3, CH(CH3)CH2CD3, CH2CH(CH3)CH3, CH2CH(CH3)CY3, CH2CH(CH3)CD3, CH2C(CH3)3, CH2C(CY3)3, CH2C(CD3)3, CH2CH2C(CH3)3, CH2CH2C(CY3)3, and CH2CH2C(CD3)3, including any member, combination, or subset thereof, wherein each Y is independently a halogen atom. In some embodiments, each Y is optionally and independently selected from F, Cl, Br, and I. In some embodiments, each Y is optionally and independently selected from F, Cl, and Br. In some embodiments, each Y is optionally and independently selected from F, Cl, and I. In some embodiments, each Y is optionally and independently selected from F, Br, and I. In some embodiments, each Y is optionally andindependently selected from Cl, Br, and I. In some embodiments, each Y is optionally and independently selected from F and Cl. In some embodiments, each Y is optionally and independently selected from F and Br. In some embodiments, each Y is optionally and independently selected from F and I. In some embodiments, each Y is optionally and independently selected from Cl and Br. In some embodiments, each Y is optionally and independently selected from Cl and I. In some embodiments, each Y is optionally and independently selected from Br and I. In some embodiments, each Y is F. In some embodiments, each Y is Cl. In some embodiments, each Y is Br. In some embodiments, each Y is I. In some embodiments, the alkyl groups are optionally and independently selected from CD2H, CDH2, CD3, CF2H, CFH2, CF3, CH2CH2F, CH2CF2H, CH2CF3, CHFCH3, CHFCH2F, CHFCHF2, CHFCF3, CF2CH3, CF2CH2F, CF2CHF2, CF2CF3, CH2CH2D, CH2CD2H, CH2CD3, CHDCH3, CHDCH2D, CHDCHD2, CHDCD3, CD2CH3, CD2CH2D, CD2CHD2, CD2CD3, CH2CH2CHF2, CH2CH2CFH2, CH2CH2CF3, CH2CH2CHD2, CH2CH2CDH2, CH2CH2CD3CH(CH3)2, CH(CF3)2, CH(CHF2)2, CH(CFH2)2, CH(CD3)2, CH(CHD2)2, CH(CDH2)2, C(CH3)3, C(CF3)3, C(CHF2)3, C(CFH2)3, C(CD3)3, C(CHD2)3, and C(CDH2)3, including any member, combination, or subset thereof.

[0146] In some embodiments, the alkylene groups (e.g., R1, R2, R9, R11, R13, R15, R18, and / or R19) optionally and independently comprise optionally substituted C1-C6alkylene. For example and without limitation, in some embodiments, R1is selected from optionally substituted OC1-C6alkyleneC(O)OH. and optionally substituted OC1-C6alkyleneOC1-C6alkyl.

[0147] In some embodiments, the alkylene groups are optionally and independently C1- C5alkylene. In some embodiments, the alkylene groups are optionally and independently C1- C4alkylene. In some embodiments, the alkylene groups are optionally and independently C1-C3alkylene. In some embodiments, the alkylene groups are optionally and independently C1-C2alkylene. In some embodiments, the alkylene groups are optionally and independently C2- C6alkylene. In some embodiments, the alkylene groups are optionally and independently C3- C6alkylene. In some embodiments, the alkylene groups are optionally and independently C4- C6alkylene. In some embodiments, the alkylene groups are optionally and independently C5- C6alkylene. In some embodiments, the alkylene groups are optionally and independentlyC1alkylene (i.e., methylene). In some embodiments, the alkylene groups are optionally and independently C2alkylene (i.e., ethylene). In some embodiments, the alkylene groups are optionally and independently C3alkylene (i.e., propylene). In some embodiments, the alkylene groups are optionally and independently C4alkylene (i.e., butylene). In some embodiments, thealkylene groups are optionally and independently C5alkylene (i.e., pentylene). In some embodiments, the alkylene groups are optionally and independently C6alkylene (i.e., hexylene).

[0148] In some embodiments, the alkylene groups are optionally and independently selected from any combination of the above. In some embodiments, the alkylene groups are optionally and independently substituted. In some embodiments, the alkylene groups are optionally and independently unsubstituted.

[0149] In some embodiments, none of the available hydrogen atoms of the alkylene groups are independently replaced with a halogen atom. In some embodiments, none of the available atoms of the alkylene groups are independently replaced with an alternative isotope thereof.

[0150] In some embodiments, the alkylene groups are optionally and independently selected from -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH(CH3)CH2-, -CH2CH2CH2CH2-, -CH2CH(CH3)-, - C(CH3)2-, -CH(CH3)CH2CH2-, -CH2CH(CH3)CH2-, -CH2CH2CH(CH3)-, -C(CH3)2CH2-, - CH2C(CH3)2-, -CH(CH3)CH(CH3)-, -CH2CH2CH2CH2CH2-, -CH(CH3)CH2CH2CH2-, -C(CH3)2CH2CH2-, -CH2CH(CH3)CH2CH2-, -CH2C(CH3)2CH2- -CH2CH2CH(CH3)CH2-, - CH2CH2C(CH3)2-, -CH2CH2CH2CH(CH3)-, -CH(CH3)CH(CH3)CH2-, -CH(CH3)CH2CH(CH3)-, - CH2CH(CH3)CH(CH3)-, -CH2CH2CH2CH2CH2CH2-, -CH(CH3)CH2CH2CH2CH2-, C(CH3)2CH2CH2CH2-, -CH2CH(CH3)CH2CH2CH2-, -CH2C(CH3)2CH2CH2CH2-, CH2CH2CH(CH3)CH2CH2-, -CH2CH2C(CH3)2CH2CH2-, -CH2CH2CH2CH(CH3)CH2-, CH2CH2CH2C(CH3)2CH2-, -CH2CH2CH2CH2CH(CH3)-, -CH2CH2CH2CH2C(CH3)2-, CH(CH3)CH(CH3)CH2CH2-, -CH(CH3)CH2CH(CH3)CH2-, -CH(CH3)CH2CH2CH(CH3)-, CH2CH(CH3)CH(CH3)CH2-, -CH2CH(CH3)CH2CH(CH3)-, -CH2CH2CH(CH3)CH(CH3)-,C(CH3)2CH(CH3)CH2-, -C(CH3)2CH2CH(CH3)-, -CH2C(CH3)2CH(CH3)-, -CH2CH(CH3)C(CH3)2-, and -C(CH3)2C(CH3)2-, including any member, combination, or subset thereof.

[0151] In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I), and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I). In some embodiments, one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In someembodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective chlorine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective fluorine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective chlorine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective bromine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the alkylene groups are optionally and independently replaced with one or more respective iodine atoms, and / or one or more available atoms of the alkylene groups are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0152] Available hydrogen(s) on the alkylene groups is / are optionally and independently substituted with one or more deuterium atoms and / or one or more halogen atoms. Examples include, but not limited to, -CY2-, -CHD-, -CD2-, -CDY-, -CY2CY2-, -CH2CD2-, -CD2CH2-, -CH2CHD- , -CHDCH2-, -CH2CHY-, -CHYCH2-, -CH2CY2-, -CY2CH2-, -CHYCHY-, -CHDCHY-, -CHYCHD-, - CD2CHY-, CHYCD2, -CHDCY2-, -CY2CHD-, -CY2CD2-, -CD2CY2-, -CD2CHD-, -CHDCD2-, - CD2CD2-, -CD2CD2CD2-, -CH2CD2CD2-, -CD2CH2CH2-, -CH2CH2CD2-, -CD2CD2CH2-, CH2CD2CH2-, -CH2CH2CHD-, -CHDCHDCH2-, -CH2CHDCHD-, -CD2CD(CH3)-, -CD2CHDCH2-, - CH2CD(CH3)-, -CH2CHDCH2-, -CD2CH(CH3)-, -CHDCH2CH2-, -CHDCH(CH3)-, etc., including any member, combination, or subset thereof, wherein each Y is independently a halogen atom. In some embodiments, each Y is optionally and independently selected from F, Cl, Br, and I. In someembodiments, each Y is optionally and independently selected from F, Cl, and Br. In some embodiments, each Y is optionally and independently selected from F, Cl, and I. In some embodiments, each Y is optionally and independently selected from F, Br, and I. In some embodiments, each Y is optionally and independently selected from Cl, Br, and I. In some embodiments, each Y is optionally and independently selected from F and Cl. In some embodiments, each Y is optionally and independently selected from F and Br. In some embodiments, each Y is optionally and independently selected from F and I. In some embodiments, each Y is optionally and independently selected from Cl and Br. In some embodiments, each Y is optionally and independently selected from Cl and I. In some embodiments, each Y is optionally and independently selected from Br and I. In some embodiments, each Y is F. In some embodiments, each Y is Cl. In some embodiments, each Y is Br. In some embodiments, each Y is I. In some embodiments, the alkylene groups optionally and independently do not include a halogen atom. In some embodiments, the alkylene groups optionally and independently do not include an alternative isotope. In some embodiments, the alkylene groups optionally and independently include neither a halogen atom nor an alternative isotope.

[0153] In some embodiments, R1and / or R2optionally and independently are or comprise an optionally substituted C3-C6cycloalkyl. For example and without limitation, in some embodiments, R2is an optionally substituted C3-C6cycloalkyl. In some embodiments, R2comprises an optionally substituted cycloalkyl group, such as when R2is selected from an optionally substituted OC3- C6cycloalkyl and an optionally substituted OC1-C6alkyleneC3-C6cycloalkyl.

[0154] In some embodiments, the C3-C6cycloalkyl groups (e.g., of R1and / or R2) are optionally and independently selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl, including any member, combination, or subset thereof, wherein one or more available hydrogen atoms are optionally replaced with one or more respective halogen atoms, and / or one or more available atoms are optionally replaced with one or more respective alternate isotopes thereof. In some embodiments, the cycloalkyl groups are independently unsubstituted, and in some embodiments the cycloalkyl groups are independently substituted. In some embodiments, the cycloalkyl groups optionally and independently do not include a halogen atom. In some embodiments, the cycloalkyl groups optionally and independently do not include an alternative isotope. In some embodiments, the cycloalkyl groups optionally and independently include neither a halogen atom nor an alternative isotope.

[0155] In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I), and / or one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I). In some embodiments, one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms, and / or one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective chlorine atoms, and / or one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective fluorine atoms, and / or one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective chlorine atoms, and / or one or more available atoms of the cycloalkyl groups are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0156] In some embodiments, R2is or comprises an optionally substituted heterocycloalkyl. For example and without limitation, in some embodiments, R2is an optionally substituted 5- to 6- membered heterocycloalkyl. In some embodiments, R2and R3are linked to one another to form an optionally substituted 3- to 5-membered heterocycloalkyl. In some embodiments, R2is selected from an optionally substituted 5- to 6-membered heterocycloalkyl, an optionally substituted O(5- to 6-membered) heterocycloalkyl, and an optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, including any member, combination, or subset thereof.

[0157] In some embodiments, the heterocycloalkyl (e.g., of R2or formed by the linking of R2and R3) independently comprises optionally substituted heterocyclopentyl. In some embodiments, the heterocycloalkyl independently comprises optionally substituted heterocyclohexyl.

[0158] In some embodiments, none of the available hydrogen atoms of the heterocycloalkyl (e.g., of R1or formed by the linking of R2and R3) are independently replaced with a halogen atom. In some embodiments, none of the available atoms of the heterocycloalkyl are independently replaced with an alternative isotope thereof. In some embodiments, none of the available hydrogen atoms of the heterocycloalkyl are independently replaced with a halogen atom, and none of the available atoms of the heterocycloalkyl are independently replaced with an alternative isotope thereof.

[0159] In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl (e.g., of R2or formed by the linking of R2and R3) are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I), and / or one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I). In some embodiments, one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms, and / or one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective chlorine atoms, and / or one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective fluorine atoms, and / or one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the heterocycloalkyl are optionally and independently replaced with one or morerespective chlorine atoms, and / or one or more available atoms of the heterocycloalkyl are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0160] In some embodiments, R2optionally and independently is or comprises an optionally substituted C6aryl (or phenyl). For example and without limitation, in some embodiments, R2is an optionally substituted C6aryl (or phenyl) or an optionally substituted C1-C6alkyleneC6aryl (e.g., benzyl).

[0161] In some embodiments, none of the available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl (e.g., of R2) are independently replaced with a halogen atom. In some embodiments, none of the available atoms of the optionally substituted C6aryl and the optionally substituted C1-C6alkyleneC6aryl are independently replaced with an alternative isotope thereof. In some embodiments, none of the available hydrogen atoms of the optionally substituted C6aryl and the optionally substituted C1-C6alkyleneC6aryl are independently replaced with a halogen atom, and none of the available atoms of the optionally substituted C6aryl and the optionally substituted C1-C6alkyleneC6aryl are independently replaced with an alternative isotope thereof.

[0162] In some embodiments, one or more available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl (e.g., of R2) are optionally and independently replaced with one or more respective halogen atoms (i.e. , F, Cl, Br, and / or I), and / or one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1- C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I). In some embodiments, one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1- C6alkyleneC6aryl are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms, and / or one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of theoptionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective chlorine atoms, and / or one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1- C6alkyleneC6aryl are optionally and independently replaced with one or more respective fluorine atoms, and / or one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted C6aryl or an optionally substituted C1-C6alkyleneC6aryl are optionally and independently replaced with one or more respective chlorine atoms, and / or one or more available atoms of the optionally substituted C6aryl or an optionally substituted C1- C6alkyleneC6aryl are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0163] In some embodiments, R2optionally and independently is or comprises an optionally substituted 5- to 6-membered heteroaryl. For example and without limitation, in some embodiments, R2is selected from an optionally substituted 5- to 6-membered heteroaryl and an optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl.

[0164] In some embodiments, none of the available hydrogen atoms of the heteroaryl (e.g., of R2) are independently replaced with a halogen atom. In some embodiments, none of the available atoms of the heteroaryl are independently replaced with an alternative isotope thereof. In some embodiments, none of the available hydrogen atoms of the heteroaryl are independently replaced with a halogen atom, and none of the available atoms of the heteroaryl are independently replaced with an alternative isotope thereof.

[0165] In some embodiments, one or more available hydrogen atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6- membered) heteroaryl (e.g., of R2) are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I), and / or one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of theoptionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective halogen atoms (i.e., F, Cl, Br, and / or I). In some embodiments, one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective fluorine atoms, one or more respective chlorine atoms, and / or one or more respective bromine atoms, and / or one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted 5- to 6- membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective chlorine atoms, and / or one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6- membered) heteroaryl are optionally and independently replaced with one or more respective fluorine atoms, and / or one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof. In some embodiments, one or more available hydrogen atoms of the optionally substituted 5- to 6- membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective chlorine atoms, and / or one or more available atoms of the optionally substituted 5- to 6-membered heteroaryl or optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl are optionally and independently replaced with one or more respective alternative isotopes thereof.

[0166] In some embodiments, all of R1, R2, R3, and R4are H not replaced by halogen atoms or alternative isotopes thereof. In some embodiments, all of R1, R2, R3, and R4are D. In some embodiments, all of R1, R2, R3, and R4are selected from H and D. In some embodiments, all ofR1, R2, R3, and R4are selected from H, D, and halo. In some embodiments, three of R1, R2, R3, and R4are H not replaced by halogen atoms or alternative isotopes thereof, and the other is not H. In some embodiments, three of R1, R2, R3, and R4are D, and the other is not D. In some embodiments, three of R1, R2, R3, and R4are selected from H and D, and the other is not H or D. In some embodiments, three of R1, R2, R3, and R4are selected from H, D, and halo, and the other is not H, D, or halo. In some embodiments, two of R1, R2, R3, and R4are H not replaced by halogen atoms or alternative isotopes thereof, and the other two are not H. In some embodiments, two of R1, R2, R3, and R4are D, and the other two are not D. In some embodiments, two of R1, R2, R3, and R4are selected from H and D, and the other two are not selected from H and D. In some embodiments, two of R1, R2, R3, and R4are selected from H, D, and halo, and the other two are not selected from H, D, and halo. In some embodiments, one of R1, R2, R3, and R4is H not replaced by a halogen atom or an alternative isotopes thereof, and the other three are not H. In some embodiments, one of R1, R2, R3, and R4is D, and the other three are not D. In some embodiments, one of R1, R2, R3, and R4is selected from H and D, and the other three are not selected from H and D. In some embodiments, one of R1, R2, R3, and R4is selected from H, D, and halo, and the other three are not selected from H, D, and halo. In some embodiments, none of R1, R2, R3, and R4are H not replaced by halogen atoms or alternative isotopes thereof. In some embodiments, none of R1, R2, R3, and R4are D. In some embodiments, none of R1, R2, R3, and R4are selected from H and D. In some embodiments, none of R1, R2, R3, and R4are selected from H, D, and halo.

[0167] According to an embodiment, the compound is selected from one or more of the following compounds of Table 1 below.

[0168] Table 1or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0169] According to another embodiment, the compound is selected from one or more of the following compounds of Table 2 below.

[0170] Table 2or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0171] According to another embodiment, the compound is selected from one or more of the following compounds of Table 3 below.

[0172] Table 3

[0173] According to another embodiment, the compound is selected from one or more of the following compounds of Table 4 below.

[0174] Table 4

[0175] According to another embodiment, the compound is selected from one or more of the following compounds of Table 5 below.

[0176] Table 5or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0177] In some embodiments of the Tables above, one or more hydrogen atoms are optionally and independently replaced with one or more respective halogen atoms, and one or moreavailable atoms are optionally and independently replaced with one or more respective isotope atoms

[0178] Some embodiments related to pharmaceutically acceptable salts, solvates, and / or prodrugs of compounds disclosed herein.

[0179] In some embodiments, the pharmaceutically acceptable salt is an acid addition salt or a base addition salt. The selection of a suitable salt may be made by a person skilled in the art. Suitable salts include acid addition salts that may, for example, be formed by mixing a solution of a compound with a solution of a pharmaceutically acceptable acid, such as hydrochloric acid, sulfuric acid, acetic acid, trifluoroacetic acid, or benzoic acid. Additionally, acids that are generally considered suitable for the formation of pharmaceutically useful salts from basic pharmaceutical compounds are discussed, for example, by P. Stahl et al., Camille G. (eds.) and Handbook of Pharmaceutical Salts. Properties, Selection and Use. (2002) Zurich: Wiley VCH; S. Berge et al., Journal of Pharmaceutical Sciences 1977 66(1) 1-19; P. Gould, International J. of Pharmaceutics (1986) 33201-217; Anderson etal., The Practice of Medicinal Chemistry (1996), Academic Press, New York; and in The Orange Book (Food and Drug Administration, Washington, D.C. on their website).

[0180] An acid addition salt suitable for, or compatible with, the treatment of subjects is any non-toxic organic or inorganic acid addition salt of any basic compound. Basic compounds that form an acid addition salt include, for example, compounds comprising an amine group. Illustrative inorganic acids which form suitable salts include hydrochloric, hydrobromic, sulfuric, nitric and phosphoric acids, as well as acidic metal salts, such as sodium monohydrogen orthophosphate and potassium hydrogen sulfate. Illustrative organic acids which form suitable salts include mono-, di-, and tricarboxylic acids. Illustrative of such organic acids are, for example, acetic, trifluoroacetic, propionic, glycolic, lactic, pyruvic, malonic, succinic, glutaric, fumaric, malic, tartaric, citric, ascorbic, maleic, hydroxymaleic, benzoic, hydroxybenzoic, phenylacetic, cinnamic, mandelic, salicylic, 2-phenoxybenzoic, p-toluenesulfonic acid, and other sulfonic acids, such as methanesulfonic acid, ethanesulfonic acid, and 2-hydroxyethanesulfonic acid. In some embodiments, exemplary acid addition salts also include acetates, ascorbates, besylates, gentisates, benzoates, benzenesulfonates, bisulfates, borates, butyrates, citrates, camphorates, camphorsulfonates, fumarates, hydrochlorides, hydrobromides, hydroiodides, lactates, maleates, methanesulfonates (“mesylates”), naphthalenesulfonates, nitrates, oxalates, phosphates, propionates, salicylates, succinates, sulfates, tartarates, thiocyanates, toluenesulfonates (alsoknown as tosylates), and the like. In some embodiments, the mono- or di-acid salts are formed and such salts exist in either a hydrated, solvated, or substantially anhydrous form. In general, acid addition salts are more soluble in water and various hydrophilic organic solvents and generally demonstrate higher melting points in comparison to their free base forms. The selection criteria for the appropriate salt will be known to one skilled in the art. Other non-pharmaceutically acceptable salts, such as, but not limited to, oxalates may be used, for example in the isolation of compounds of the disclosure for laboratory use, or for subsequent conversion to a pharmaceutically acceptable acid addition salt.

[0181] A base addition salt suitable for, or compatible with, the treatment of subjects is any nontoxic organic or inorganic base addition salt of any acidic compound. Acidic compounds that form a basic addition salt include, for example, compounds comprising a carboxylic acid group. Illustrative inorganic bases which form suitable salts include lithium, sodium, potassium, calcium, magnesium, or barium hydroxide as well as ammonia. Illustrative organic bases which form suitable salts include aliphatic, alicyclic, or aromatic organic amines, such as isopropylamine, methylamine, trimethylamine, picoline, diethylamine, triethylamine, tripropylamine, ethanolamine, 2-dimethylaminoethanol, 2-diethylaminoethanol, dicyclohexylamine, lysine, arginine, histidine, caffeine, procaine, hydrabamine, choline, betaine, ethylenediamine, glucosamine, methylglucamine, theobromine, purines, piperazine, piperidine, N-ethylpiperidine, polyamine resins, and the like. Exemplary organic bases are isopropylamine, diethylamine, ethanolamine, trimethylamine, dicyclohexylamine, choline, and caffeine. The selection of the appropriate salt may be useful, for example, so that an ester functionality, if any, elsewhere in a compound is not hydrolyzed. The selection criteria for the appropriate salt will be known to one skilled in the art. In some embodiments, exemplary basic salts also include ammonium salts, alkali metal salts, such as sodium, lithium, and potassium salts, alkaline earth metal salts, such as calcium and magnesium salts, salts with organic bases (for example, organic amines), such as dicyclohexylamine, butyl amine, choline, and salts with amino acids, such as arginine, lysine, and the like. Basic nitrogen containing groups may be quarternized with agents, such as lower alkyl halides (e.g., methyl, ethyl, and butyl chlorides, bromides, and iodides), dialkyl sulfates (e.g., dimethyl, diethyl, and dibutyl sulfates), long chain halides (e.g., decyl, lauryl, and stearyl chlorides, bromides, and iodides), aralkyl halides (e.g., benzyl and phenethyl bromides), and others. Compounds carrying an acidic moiety can be mixed with suitable pharmaceutically acceptable salts to provide, for example, alkali metal salts (e.g., sodium or potassium salts), alkaline earth metal salts (e.g., calcium or magnesium salts), and salts formed with suitable organic ligands,such as quaternary ammonium salts. Also, in the case of an acid (-COOH) or alcohol group being present, pharmaceutically acceptable esters can be employed to modify the solubility or hydrolysis characteristics of the compound.

[0182] All such acid salts and base salts are intended to be pharmaceutically acceptable salts within the scope of the disclosure and all acid and base salts are considered equivalent to the free forms of the corresponding compounds for purposes of the disclosure. In addition, when a compound of the disclosure contains both a basic moiety, such as, but not limited to, an aliphatic primary, secondary, tertiary, or cyclic amine, an aromatic or heteroaryl amine, pyridine, or imidazole and an acidic moiety, such as, but not limited to, tetrazole or carboxylic acid, zwitterions (“inner salts”) may be formed and are included within the terms “salt(s),” as used herein. It is understood that certain compounds of the disclosure may exist in zwitterionic form, having both anionic and cationic centers within the same compound and a net neutral charge. Such zwitterions are included within the disclosure.

[0183] Solvates of compounds of the disclosure include, for example, those made with solvents that are pharmaceutically acceptable. Examples of such solvents include water (resulting solvate is called a hydrate) and ethanol and the like. Suitable solvents are physiologically tolerable at the dosage administered.

[0184] Prodrugs of the compounds of the present disclosure include, for example, conventional esters formed with available hydroxy, thiol, amino, or carboxyl groups. Some common esters which have been utilized as prodrugs are phenyl esters, aliphatic (C1-C24) esters, acyloxymethyl esters, carbamates, and amino acid esters.

[0185] It is understood and appreciated that in some embodiments, compounds of the present disclosure may have at least one chiral center and therefore can exist as enantiomers and / or diastereomers. It is to be understood that all such isomers and mixtures thereof in any proportion are encompassed within the scope of the present disclosure. It is to be further understood that while the stereochemistry of the compounds may be as shown in any given compound listed herein, such compounds may also contain certain amounts (for example, less than 20%, suitably less than 10%, more suitably less than 5%) of compounds of the present disclosure having an alternate stereochemistry. It is intended that any optical isomers, as separated, pure, or partially purified optical isomers or racemic mixtures thereof are included within the scope of the present disclosure.

[0186] In some embodiments, the compounds of the present disclosure can also include tautomeric forms. Tautomeric forms can be in equilibrium or sterically locked into one form by appropriate substitution. It is intended that any tautomeric forms which the compounds form, as well as mixtures thereof, are included within the scope of the present disclosure.

[0187] The compounds of the present disclosure may further exist in varying amorphous and polymorphic forms and it is contemplated that any amorphous forms, polymorphs, or mixtures thereof, which form are included within the scope of the present disclosure.

[0188] In the compounds of general Formula (I) and pharmaceutically acceptable salts, solvates, and / or prodrugs thereof, the atoms may exhibit their natural isotopic abundances, or one or more of the atoms may be artificially enriched in a particular isotope having the same atomic number, but an atomic mass or mass number different from the atomic mass or mass number predominantly found in nature. The present disclosure is meant to include all suitable isotopic variations of the compounds of the disclosure and pharmaceutically acceptable salts, solvates, and / or prodrugs thereof. For example, different isotopic forms of hydrogen (H) include protium (1 H), deuterium (2H), and tritium (3H). Protium is the predominant hydrogen isotope found in nature.

[0189] The compounds of the present disclosure may further be radiolabeled and accordingly all radiolabeled versions of the compounds of the disclosure are included within the scope of the present disclosure. Therefore, the compounds of the disclosure also include those in which one or more radioactive atoms are incorporated within their structure.III. Compositions

[0190] The compounds of the present disclosure are suitably formulated in a conventional manner into compositions using one or more carriers. Accordingly, the present disclosure also includes a composition comprising one or more compounds of the disclosure and a carrier. The compounds of the disclosure are suitably formulated into pharmaceutical compositions for administration to subjects in a biologically compatible form suitable for administration in vivo. Accordingly, the present disclosure further includes a pharmaceutical composition comprising one or more compounds of the disclosure and a pharmaceutically acceptable carrier. In embodiments of the disclosure the pharmaceutical compositions are used in the treatment of any of the diseases, disorders, or conditions described herein.

[0191] In embodiments, compounds and / or compositions of the disclosure are administered to a subject in one or more of a variety of forms depending on the selected route of administration, as will be understood by those skilled in the art. For example, a compound and / or composition of the disclosure is administered by oral, inhalation, parenteral, buccal, sublingual, insufflation, epidurally, nasal, rectal, vaginal, patch, pump, minipump, topical, or transdermal administration and the pharmaceutical compositions formulated accordingly. In some embodiments, administration is by means of a pump for periodic or continuous delivery. Conventional procedures and ingredients for the selection and preparation of suitable compositions are described, for example, in Remington's Pharmaceutical Sciences (2000 - 20th edition) and in The United States Pharmacopeia: The National Formulary (USP 24 NF19) published in 1999.

[0192] Parenteral administration includes systemic delivery routes other than the gastrointestinal (Gl) tract and includes, for example intravenous, intra-arterial, intraperitoneal, subcutaneous, intramuscular, transepithelial, nasal, intrapulmonary (for example, by use of an aerosol), intrathecal, rectal, and topical (including the use of a patch or other transdermal delivery device) modes of administration. Parenteral administration may be by continuous infusion over a selected period of time.

[0193] In some embodiments, a compound and / or composition of the disclosure is orally administered, for example, with an inert diluent or with an assimilable edible carrier, or it is enclosed in hard- or soft-shell gelatin capsules, or it is compressed into tablets, or it is incorporated directly with the food of the diet. In some embodiments, the compound and / or composition is incorporated with excipient(s) and used in the form of ingestible tablets, buccal tablets, troches, capsules, caplets, pellets, granules, lozenges, chewing gum, powders, syrups, elixirs, wafers, aqueous solutions, suspensions, and the like. In the case of tablets, carriers that are used include lactose, com starch, sodium citrate, and salts of phosphoric acid. Pharmaceutically acceptable excipients include binding agents (e.g., pregelatinized maize starch, polyvinylpyrrolidone, or hydroxypropyl methylcellulose); fillers (e.g., lactose, microcrystalline cellulose, or calcium phosphate); lubricants (e.g., magnesium stearate, talc, or silica); disintegrants (e.g., potato starch or sodium starch glycolate); wetting agents (e.g., sodium lauryl sulphate); and / or solvents (e.g., medium chain triglycerides, ethanol, or water). In embodiments, the tablets are coated by methods well known in the art. In the case of tablets, capsules, caplets, pellets, or granules for oral administration, pH sensitive enteric coatings, such as Eudragits™, designed to control the release of active ingredients are optionally used. Oral dosage forms also include modified release, for example immediate release and timed-release, formulations.Examples of modified-release formulations include, for example, sustained-release (SR), extended-release (ER, XR, or XL), time-release or timed-release, controlled-release (CR), or continuous-release (CR or Contin), employed, for example, in the form of a coated tablet, an osmotic delivery device, a coated capsule, a microencapsulated microsphere, an agglomerated particle, e.g., as of molecular sieving type particles, or, a fine hollow permeable fiber bundle, or chopped hollow permeable fibers, agglomerated or held in a fibrous packet. Timed-release compositions are formulated, for example, as liposomes or those wherein the active compound is protected with differentially degradable coatings, such as by microencapsulation, multiple coatings, etc. Liposome delivery systems include, for example, small unilamellar vesicles, large unilamellar vesicles, and multilamellar vesicles. In some embodiments, liposomes are formed from a variety of phospholipids, such as cholesterol, stearylamine, or phosphatidylcholines. For oral administration in a capsule form, useful carriers, solvents, or diluents include lactose, medium chain triglycerides, ethanol, and dried corn starch.

[0194] In some embodiments, liquid preparations for oral administration take the form of, for example, solutions, syrups, or suspensions, or they are suitably presented as a dry product for constitution with water or other suitable vehicle before use. When aqueous suspensions and / or emulsions are administered orally, the compound of the disclosure is suitably suspended or dissolved in an oily phase that is combined with emulsifying and / or suspending agents. If desired, certain sweetening and / or flavoring and / or coloring agents are added. Such liquid preparations for oral administration are prepared by conventional means with pharmaceutically acceptable additives, such as suspending agents (e.g., sorbitol syrup, methyl cellulose, or hydrogenated edible fats); emulsifying agents (e.g., lecithin or acacia); non-aqueous vehicles (e.g., medium chain triglycerides, almond oil, oily esters, or ethyl alcohol); and / or preservatives (e.g., methyl or propyl p-hydroxybenzoates or sorbic acid). Useful diluents include lactose and high molecular weight polyethylene glycols.

[0195] It is also possible to freeze-dry the compounds of the disclosure and use the lyophilizates obtained, for example, for the preparation of products for injection.

[0196] In some embodiments, a compound and / or composition of the disclosure is administered parenterally. For example, solutions of a compound of the disclosure are prepared in water suitably mixed with a surfactant, such as hydroxypropylcellulose. In some embodiments, dispersions are prepared in glycerol, liquid polyethylene glycols, DMSO, and mixtures thereof with or without alcohol and in oils. Under ordinary conditions of storage and use, these preparationscontain a preservative to prevent the growth of microorganisms. A person skilled in the art would know how to prepare suitable formulations. For parenteral administration, sterile solutions of the compounds and / or compositions of the disclosure are usually prepared and the pHs of the solutions are suitably adjusted and buffered. For intravenous use, the total concentration of solutes should be controlled to render the preparation isotonic. For ocular administration, ointments, or droppable liquids are delivered, for example, by ocular delivery systems known to the art, such as applicators or eye droppers. In some embodiments, such compositions include mucomimetics, such as hyaluronic acid, chondroitin sulfate, hydroxypropyl methylcellulose, or polyvinyl alcohol, preservatives, such as sorbic acid, EDTA, or benzyl chromium chloride, and the usual quantities of diluents or carriers. For pulmonary administration, diluents or carriers will be selected to be appropriate to allow the formation of an aerosol.

[0197] In some embodiments, a compound and / or composition of the disclosure is formulated for parenteral administration by injection, including using conventional catheterization techniques or infusion. Formulations for injection are, for example, presented in unit dosage form, e.g., in ampoules or in multi-dose containers, with an added preservative. In some embodiments, the compositions take such forms as sterile suspensions, solutions, or emulsions in oily or aqueous vehicles and contain formulating agents, such as suspending, stabilizing, and / or dispersing agents. In all cases, the form must be sterile and must be fluid to the extent that easy syringability exists. Alternatively, the compounds and / or compositions of the disclosure are suitably in a sterile powder form for reconstitution with a suitable vehicle, e.g., sterile pyrogen-free water, before use.

[0198] In some embodiments, compositions for nasal administration are conveniently formulated as aerosols, drops, gels, and powders. For intranasal administration or administration by inhalation, the compounds of the disclosure are conveniently delivered in the form of a solution, dry powder formulation, or suspension from a pump spray container that is squeezed or pumped by the patient or as an aerosol spray presentation from a pressurized container or a nebulizer. Aerosol formulations typically comprise a solution or fine suspension of the active substance in a physiologically acceptable aqueous or non-aqueous solvent and are usually presented in single or multidose quantities in sterile form in a sealed container, which, for example, take the form of a cartridge or refill for use with an atomizing device. Alternatively, the sealed container is a unitary dispensing device, such as a single dose nasal inhaler or an aerosol dispenser fitted with a metering valve which is intended for disposal after use. Where the dosage form comprises an aerosol dispenser, it will contain a propellant which is, for example, a compressed gas, such as compressed air, or an organic propellant, such as fluorochlorohydrocarbon. Suitable propellantsinclude but are not limited to dichlorodifluoromethane, trichlorofluoromethane, dichlorotetrafl uoroethane, heptafluoroalkanes, carbon dioxide, or another suitable gas. In the case of a pressurized aerosol, the dosage unit is suitably determined by providing a valve to deliver a metered amount. In some embodiments, the pressurized container or nebulizer contains a solution or suspension of the active compound. Capsules and cartridges (made, for example, from gelatin) for use in an inhaler or insufflator are, for example, formulated containing a powder mix of a compound and / or composition of the disclosure and a suitable powder base, such as lactose or starch. The aerosol dosage forms can also take the form of a pump-atomizer.

[0199] Compositions suitable for buccal or sublingual administration include tablets, lozenges, and pastilles, wherein a compound of the disclosure is formulated with a carrier, such as sugar, acacia, tragacanth, or gelatin, and glycerine. Compositions for rectal administration are conveniently in the form of suppositories containing a conventional suppository base, such as cocoa butter.

[0200] Suppository forms of the compounds and / or compositions of the disclosure are useful for vaginal, urethral, and rectal administrations. Such suppositories will generally be constructed of a mixture of substances that is solid at room temperature but melts at body temperature. The substances commonly used to create such vehicles include but are not limited to theobroma oil (also known as cocoa butter), glycerinated gelatin, other glycerides, hydrogenated vegetable oils, mixtures of polyethylene glycols of various molecular weights and fatty acid esters of polyethylene glycol. See, for example: Remington's Pharmaceutical Sciences, 16th Ed., Mack Publishing, Easton, PA, 1980, pp. 1530-1533 for further discussion of suppository dosage forms.

[0201] In some embodiments, a compound of the disclosure is coupled with soluble polymers as targetable drug carriers. Such polymers include, for example, polyvinylpyrrolidone, pyran copolymer, polyhydroxypropylmethacrylamide-phenol, polyhydroxy-ethylaspartamide-phenol, or polyethyleneoxide-polylysine substituted with palmitoyl residues. Furthermore, in some embodiments, a compound of the disclosure is coupled to a class of biodegradable polymers useful in achieving controlled release of a drug, for example, polylactic acid, polyglycolic acid, copolymers of polylactic and polyglycolic acid, polyepsilon caprolactone, polyhydroxy butyric acid, polyorthoesters, polyacetals, polydihydropyrans, polycyanoacrylates, and crosslinked or amphipathic block copolymers of hydrogels.

[0202] Compounds of the disclosure including pharmaceutically acceptable salts, solvates, and / or prodrugs thereof are suitably used on their own but will generally be administered in the form of a pharmaceutical composition in which the one or more compounds of the disclosure (the active ingredient) is in association with a pharmaceutically acceptable carrier. Depending on the mode of administration, the pharmaceutical composition will comprise from about 0.05 wt% to about 99 wt%, or about 0.10 wt% to about 70 wt%, of the active ingredient and from about 1 wt% to about 99.95 wt%, or about 30 wt% to about 99.90 wt% of a pharmaceutically acceptable carrier, all percentages by weight being based on the total composition.

[0203] In some embodiments, the compounds of the disclosure including pharmaceutically acceptable salts, solvates, and / or prodrugs thereof are used are administered in a composition comprising an additional therapeutic agent. Therefore, the present disclosure also includes a pharmaceutical composition comprising one or more compounds of the disclosure, or pharmaceutically acceptable salts, solvates, and / or prodrugs thereof and an additional therapeutic agent, and optionally one or more pharmaceutically acceptable excipients. In some embodiments, the additional therapeutic agent is another known agent useful for treatment of a disease, disorder, or condition, for example those listed in the Methods and Uses section below.

[0204] In the above, the term “a compound" also includes embodiments wherein one or more compounds are referenced.IV. Methods and Uses of the Disclosure

[0205] Compounds and / or compositions disclosed herein may be administered alone or in combination with other compounds and / or compositions to treat a wide range of disorders, diseases, and conditions that include, but are not limited to, depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, burnout, and a combination thereof.

[0206] The compounds and / or compositions of the present disclosure are useful as medicaments. Accordingly, the disclosure also includes a compound and / or a composition of the disclosure for use as, among other things, a medicament.

[0207] The present disclosure also includes a method of treating a disease, disorder, or condition by administering a therapeutically effective amount of one or more compounds and / or compositions of the disclosure to a subject in need thereof. The present disclosure also includes use of one or more compounds and / or compositions of the disclosure to manufacture a medicine or medicament that in a therapeutically effect amount treats a disease, disorder, or condition.

[0208] The present disclosure also includes use of one or more compounds and / or compositions of the disclosure for treatment of a disease, disorder, or condition as well as use of one or more compounds and / or compositions of the disclosure for the preparation and manufacture of a medicine or medicament for treatment of a disease, disorder, or condition.

[0209] In some embodiments, the compounds and / or compositions of the disclosure are useful for preventing, treating, and / or reducing the severity of a disease, disorder, and / or condition in a subject. Accordingly, the present disclosure also includes a method of preventing, treating, and / or reducing the severity of a disease, disorder, and / or condition comprising administering a therapeutically effective amount of one or more compounds and / or compositions of the disclosure to a subject in need thereof. The present disclosure also includes use of one or more compounds and / or compositions of the disclosure for treatment a disease, disorder, and / or condition, as well as use of one or more compounds and / or compositions of the disclosure for the preparation of a medicament for preventing, treating, and / or reducing the severity of a disease, disorder, and / or condition in a subject.

[0210] Some embodiments disclosed herein are directed to a method of treating a depressive disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the depressive disorder is selected from major depressive disorder (MDD), MDD with suicidal ideation, persistent depressive disorder, dysthymia, dysthymic disorder, seasonal affective disorder, pre-menstrual dysphoric disorder, antenatal depression, postpartum depression, postnatal depression, treatment-resistant depression, depression related to a medical condition, depression in bipolar disorder, depression related to substance use, depression related to medicine use, psychotic depression, and a combination thereof.

[0211] Some embodiments disclosed herein are directed to a method of treating a bipolar disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the bipolar disorder is selected from Bipolar I disorder, Bipolar II disorder, cyclothymia, cyclothymic disorder, bi-polar related to a medicinal condition, and a combination thereof.

[0212] Some embodiments disclosed herein are directed to a method of treating an eating disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the eating disorder is selected from anorexia nervosa, bulimia nervosa, avoidant restrictive food intake disorder, other specified feeding and eating disorders, pica, rumination disorder, avoidant / restrictive food intake disorder, and a combination thereof.

[0213] Some embodiments disclosed herein are directed to a method of treating an impulsecontrol disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the impulse-control disorder is selected from binge-eating disorder, obsessive compulsive disorder, and a combination thereof.

[0214] Some embodiments disclosed herein are directed to a method of treating a personality disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the personality disorder is selected from avoidant personality disorder, dependent personality disorder, borderline personality disorder, histrionic personality disorder, narcissistic personality disorder, paranoid personality disorder, and a combination thereof.

[0215] Some embodiments disclosed herein are directed to a method of treating a substance use / abuse and / or behavioral addiction disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the substance use / abuse and / or behavioral addiction disorder is selected from alcohol use disorder, stimulant use disorder, cannabis use disorder, opioid use disorder, tobacco use disorder, nicotine use disorder, inhalant use disorder, sedativehypnotic use disorder, anxiolytic use disorder, gambling disorder, gaming disorder, compulsive sexual behavior disorder, and a combination thereof.

[0216] Some embodiments disclosed herein are directed to a method of treating an anxiety and / or stress disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the anxiety disorder and / or the stress disorder is selected from acute stress disorder, adjustment disorder in chronic illness, body dysmorphic disorder, generalized anxiety disorder, panic disorder, post-traumatic stress disorder, prolonged grief disorder, social anxiety disorder, agoraphobia, separation anxiety disorder, specific phobias, anxiety due to a medical condition, anxiety in advanced stage illness, selective mutism, and a combination thereof.

[0217] Some embodiments disclosed herein are directed to a method of treating a neurodevelopmental disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the neurodevelopmental disorder is selected from attention deficit hyperactivity disorder and subtypes, autism spectrum disorder, behavioral symptoms of Fragile X syndrome, and a combination thereof.

[0218] Some embodiments disclosed herein are directed to a method of treating a pain disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the pain disorder is selected from fibromyalgia, neuropathic pain, phantom limb pain, chronic pain, and a combination thereof.

[0219] Some embodiments disclosed herein are directed to a method of treating a headache disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the headache disorder is selected from cluster headaches, short-lasting unilateral neuralgiform headaches, tension-type headaches, chronic daily headache syndrome, migraine headaches, and a combination thereof.

[0220] Some embodiments disclosed herein are directed to a method of treating an inflammatory disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the inflammatory disorder is selected from inflammatory bowel disease, multiple sclerosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, system lupus erythematosus, systemic sclerosis, vasculitis, and a combination thereof.

[0221] Some embodiments disclosed herein are directed to a method of treating an injury- related disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the injury-related disorder is selected from cognitive and / or behavioral symptoms of TBI, functional recovery in stroke, or a combination thereof.

[0222] Some embodiments disclosed herein are directed to a method of treating a neurodegenerative disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the neurodegenerative disorder is selected from Alzheimer's disease, amyotrophic lateral sclerosis (ALS), behavioral symptoms in ALS, frontotemporal dementia, Parkinson’s disease, vascular dementia, Huntington’s disease, and a combination thereof.

[0223] Some embodiments disclosed herein are directed to a method of treating a functional disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the functional disorder is selected from chronic fatigue syndrome, functional neurological disorder, irritable bowel syndrome, long COVID, post-treatment Lyme, and a combination thereof.

[0224] Some embodiments disclosed herein are directed to a method of treating a psychotic disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the psychotic disorder is selected from schizophrenia, delusional disorder, schizoaffective disorder, and a combination thereof.

[0225] Some embodiments disclosed herein are directed to a method of treating a hyperkinetic disorder comprising administering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof. In some embodiments, the hyperkinetic movement disorder is selected from chorea, akathisia, asterixis, dystonia, tremor, myoclonus, tics, stereotypies, movement disorders caused by neurodegenerative disease, metabolic derangements, vascular and autoimmune disease, infections, medications, recreational drugs, and / or pregnancy, and a combination thereof.

[0226] The present disclosure also includes a method of treating age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout, comprisingadministering a therapeutically effective amount of one or more compounds and / or compositions disclosed herein to a subject in need thereof.

[0227] In some embodiments, the subject is a non-human mammal. In other embodiments, the subject is human. Accordingly, the compounds, compositions, methods, and uses of the present disclosure are directed to human and non-human diseases, disorders, and conditions.

[0228] In some embodiments, the “subject in need thereof’ is a subject having the disease, disorder, or condition to be treated.

[0229] The present disclosure also includes a method of treating a disease, disorder, or condition comprising administering a therapeutically effective amount of one or more compounds and / or compositions of the disclosure in combination with another known agent useful for treatment of a disease, disorder, or condition to a subject in need thereof. The present disclosure also includes use of one or more compounds and / or compositions of the disclosure in combination with another known agent useful for treatment of a disease, disorder, or condition for treatment of a disease, disorder, or condition, as well as use of one or more compounds and / or compositions of the disclosure in combination with another known agent useful for treatment of a disease, disorder, or condition for the preparation of a medicament for treatment of a disease, disorder, or condition. The disclosure further includes one or more compounds and / or compositions of the disclosure in combination with another known agent useful for treatment of a disease, disorder, or condition for use in treating a disease, disorder, or condition.

[0230] In some embodiments, the one or more compounds and / or compositions of the disclosure are administered in combination with one or more additional treatments for a disease, disorder, or condition.

[0231] In some embodiments, the one or more compounds and / or compositions of the disclosure are administered in combination with one or more additional medicaments for the treatment of the disease, disorder, or condition.

[0232] In some embodiments, effective amounts vary according to factors such as the disease state, age, sex, and / or weight of the subject or species. In some embodiments, the amount of a given compound or compounds that will correspond to an effective amount will vary depending upon factors, such as the given drug(s) or compound(s), the pharmaceutical formulation, the routeof administration, the type of condition, disease, or disorder, the identity of the subject being treated, and the like, but can nevertheless be routinely determined by one skilled in the art.

[0233] In some embodiments, the compounds and / or compositions of the disclosure are administered one, two, three, or four times a year. In some embodiments, the compounds and / or compositions of the disclosure are administered at least once a week. However, in another embodiment, the compounds and / or compositions are administered to the subject from about one time per one week, two weeks, three weeks, or one month. In another embodiment, the compounds and / or compositions are administered about once per week to about once daily. In another embodiment, the compounds and / or compositions are administered 1 , 2, 3, 4, 5, or 6 times daily. The length of the treatment period depends on a variety of factors, such as the severity of the disease, disorder, or condition, the age of the subject, the concentration and / or the activity of the compounds and / or compositions of the disclosure and / or a combination thereof. It will also be appreciated that the effective dosage of the compound used for the treatment may increase or decrease over the course of a particular treatment regime. Changes in dosage may result and become apparent by standard diagnostic assays known in the art. In some instances, chronic administration is required. For example, the compounds and / or compositions are administered to the subject in an amount and for duration sufficient to treat the subject.

[0234] In some embodiments, the compounds and / or compositions of the disclosure are administered at doses that may occur once, twice, three, or four times a year. However, in some embodiments, the compounds and / or compositions are administered to the subject once daily, once every two days, once every 3 days, once a week, once every two weeks, once a month, once every two months, or once every three months at doses.

[0235] A compound and / or composition of the disclosure is either used alone or in combination with other known agent(s) useful for treating diseases, disorders, or conditions. When used in combination with other known agents useful in treating diseases, disorders, or conditions, it is an embodiment that a compound and / or composition of the disclosure is administered contemporaneously with those agents. As used herein, “contemporaneous administration" of two substances to a subject means providing each of the two substances so that they are both active in the individual at the same time. The exact details of the administration will depend on the pharmacokinetics of the two substances in the presence of each other and can include administering the two substances within a few hours of each other, or even administering one substance within 24 hours of administration of the other, if the pharmacokinetics are suitable. Thedesign of suitable dosing regimens is routine for one skilled in the art. In particular embodiments, two substances will be administered substantially simultaneously, i.e., within minutes of each other, or in a single composition that contains both substances. It is a further embodiment of the present disclosure that a combination of agents is administered to a subject in a noncontemporaneous fashion. In some embodiments, a compound and / or composition of the present disclosure is administered with another therapeutic agent simultaneously or sequentially in separate unit dosage forms or together in a single unit dosage form. Accordingly, the present disclosure provides a single unit dosage form comprising one or more compounds of the disclosure, an additional therapeutic agent and / or a pharmaceutically acceptable carrier.

[0236] The dosage of a compound and / or composition of the disclosure varies depending on many factors, such as the pharmacodynamic properties of the compound, the mode of administration, the age, health, and weight of the recipient, the nature and extent of the symptoms, the frequency of the treatment, and the type of concurrent treatment, if any, and the clearance rate of the compound in the subject to be treated. One of skill in the art can determine the appropriate dosage based on the above factors. In some embodiments, one or more compounds and / or compositions of the disclosure are administered initially in a suitable dosage that is adjusted as required, depending on the clinical response. Dosages will generally be selected to maintain a serum level of the one or more compounds of the disclosure from about 0.01 μg / cc to about 1000 μg / cc, or about 0.1 μg / cc to about 100 μg / cc. As a representative example, oral dosages of one or more compounds of the disclosure may range between about 10 μg per day to about 1000 mg per day for an adult, suitably about 10 μg per day to about 500 mg per day, more suitably about 10 μg per day to about 200 mg per day. For parenteral administration, a representative amount is from about 0.0001 mg / kg to about 10 mg / kg, about 0.0001 mg / kg to about 1 mg / kg, about 0.01 mg / kg to about 0.1 mg / kg, or about 0.0001 mg / kg to about 0.01 mg / kg may be administered. For oral administration, a representative amount may be from about 0.001 μg / kg to about 10 mg / kg, about 0.1 μg / kg to about 10 mg / kg, about 0.01 μg / kg to about 1 mg / kg, or about 0.1 μg / kg to about 1 mg / kg. For administration in suppository form, a representative amount is from about 0.1 mg / kg to about 10 mg / kg or about 0.1 mg / kg to about 1 mg / kg. In some embodiments of the disclosure, compositions are formulated for oral administration and the one or more compounds are suitably in the form of tablets containing, for example, 0.1, 0.25, 0.5, 0.75, 1.0, 5.0, 10.0, 20.0, 25.0, 30.0, 40.0, 50.0, 60.0, 70.0, 75.0, 80.0, 90.0, 100.0, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, or 1000 mg of active ingredient (one or more compounds of the disclosure) per tablet. In some embodiments of the disclosurethe one or more compounds of the disclosure are administered in a single daily, weekly, or monthly dose or the total daily dose is divided into two, three, or four daily doses.

[0237] To be clear, in the above, the term “a compound” also includes embodiments wherein one or more compounds are referenced. Likewise, the term “compounds of the disclosure” also includes embodiments wherein only one compound is referenced.V. Preparation of Compounds

[0238] Compounds of the present disclosure can be synthesized by various synthetic processes. The choice of particular structural features and / or substituents may influence the selection of one process over another. The selection of a particular process to prepare a given compound of the disclosure is within the purview of the person of skill in the art. Some starting materials for preparing compounds of the present disclosure are available from commercial chemical sources or may be extracted from cells, plants, animals, or fungi. Other starting materials, for example as described below, are readily prepared from available precursors using straightforward transformations that are well known in the art. In the Schemes below showing some embodiments of methods of preparation of compounds of the disclosure, all variables are as defined in Formula (I), unless otherwise stated.

[0239] In some embodiments of the application, the compounds of the application are generally prepared according to the process illustrated in Schemes 1-4.

[0240] In some embodiments, the compounds of Formula (I) wherein R6and R7are H or D are prepared by reduction of the corresponding indole compound A, wherein R1, R2, R3, R4, and R5are as defined in Formula (I), as shown in Scheme 1 :

[0241] In some embodiments, when X is O, the reduction is performed using a silane reducing agent, such as triethyl silane in an acid such as trifluoroacetic acid, or deuterated versions thereof, using trifluoroacetic acid-d. In some embodiments, the reaction is made enantio- ordiastereoselective via the use of chiral reducing agents or chiral auxiliaries. In some embodiments, the reduction is performed using any suitable reducing conditions known in the art, such as, for example, the reducing conditions described Larson, Gerald L.; et al. in Organic Reactions (Hoboken, NJ, United States) (2008), 71, 1-737 or the Birch type reduction as described by Lei et al. in Org. Lett. 2018, 20, 3439-3442. In some embodiments when X is S, the reduction can be a Birch-type reduction performed in aqueous media, using tetrabutylammonium tetrafluoroborate in tetrahydrofuran and water, or using tetrabutylammonium hydroxide in water. The reducing conditions are described in Pacut, Ryszard I.; et al Journal of Organic Chemistry (1986), 51(18), 3468-70. In some embodiments when X is CR18R19or CH2, a catalytic hydrogenation can be performed in the presence of Raney nickel (Tetrahedron Letters (1986), 27(44), 5383-4) or in the presence of lead tetraacetate with hydrazine in ethanol (Heterocycles (1984), 22(6), 1369-75).

[0242] In some embodiments, compounds of Formula A are available as shown in Scheme 2:

[0243] Therefore, in some embodiments when X is O and R is H, 2-iodophenol compounds of Formula B, wherein R1, R2, R3and R4are as defined in Formula (I), are reacted with alkynes of Formula C, wherein R5and Q are as defined in Formula (I), in the presence of a copper catalyst, for example using the conditions described by Nair, Reji N. et al. in Chemistry - A European Journal (2010), 16(27), 7992-7995, to provide the compounds of Formula A. A person skilled in the art would appreciate that the reaction shown in Scheme 2 can also be used to provide compounds of Formula A by using a compound of Formula B wherein R is a suitable protecting group and removing the protecting group to provide the compound of Formula A. In some embodiments when X is S and R is H, 2-iodothiophenol compounds are reacted with alkynes of Formula C in the presence of N, N,N',N'-Tetramethylethylenediamine and Palladium diacetate catalysts and silver trifluoroacetate in dimethylformamide for example using the conditionsdescribed in Chen, Jingwen; et al. RSC Advances (2017), 7(13), 7753-7757. In some embodiments of A, when X is CR18R19or CH2a 2-iodophenyl ketone or aldehyde compound is carbocyclized with an alkyne in the presence of a cobalt catalyst and zinc powder, according the procedure of Chien-Hong Cheng et al. in J. Org. Chem (2004), 69 (14) 4781-4787.

[0244] In some embodiments, when Q is(Q4) and R16and R17are either H or D, the compounds of Formula A are prepared as shown in Scheme 3:

[0245] Therefore, in some embodiments, compounds of Formula D, wherein R1-R5are as defined in Formula (I), are reacted under basic conditions using, for example, ethyl magnesium bromide with compounds of Formula F, wherein R14and p are as defined in Formula (I), R15is as defined in Formula (I) or is a suitable protecting group, and LG is a suitable leaving group, such as chloro, to provide compounds of Formula G. Reduction of keto group in the compounds of Formula G, for example using Al-based reducing agents such as lithium borohydride, lithiumaluminum hydride or lithium aluminum deuteride, provides the compounds of Formula A, wherein R16and R17are either H or D. If R15is a protecting group, it is either removed in a separate step or, wherein the protecting group is removed in the presence of Al-based reducing agents, is removed during the reduction of the compounds of Formula G.

[0246] In some embodiments, when Q is(Q1), R9, R8and m are as defined in Formula (I), the compounds of Formula A are prepared as shown in Scheme 4:

[0247] Therefore, in some embodiments, compounds of Formula D, wherein R1-R7are as defined in Formula (I), are coupled with compounds of Formula H, in a suitable solvent such as acetic acid, to provide compounds of Formula J. Reduction of the keto groups in the compounds of Formula J, for example using Al-based reducing agents such as lithium borohydride, lithiumaluminum hydride, or lithium aluminum deuteride, provides the compounds of Formula A, whereinQ is(Q1), and wherein R8, R9, and m are as defined in Formula (I). If R9is a protecting group, it is either removed in a separate step or, wherein the protecting group is removed in the presence of Al-based reducing agent(s), is removed during the reduction of the compounds of Formula J. A person skilled in the art would appreciate that a similar reaction sequence can be used to prepare compounds of Formula A, wherein Q is(Q2) or(Q3), wherein R10, R11, and “o” are as defined in Formula (I) and R12, R13, and “p” are as defined in Formula (I). R11and R13may be suitable protecting groups.

[0248] A person skilled in the art would appreciate that further manipulation of the substituent groups using known chemistry can be performed on the intermediates and final compounds in the Schemes above to provide alternative compounds of the application.

[0249] V.D. Further preparation discussion

[0250] Salts of compounds of the disclosure may be formed by methods known to those of ordinary skill in the art, for example, by reacting a compound of the disclosure with an amount of acid or base, such as an equivalent amount, in a medium, such as one in which the salt precipitates, or in aqueous medium followed by lyophilization.

[0251] The formation of solvates will vary depending on the compound and the solvate. In general, solvates are formed by dissolving the compound in the appropriate solvent and isolating the solvate by cooling or using an antisolvent. The solvate is typically dried or azeotroped under ambient conditions. The selection of suitable conditions to form a particular solvate can be made by a person skilled in the art. Examples of suitable solvents are ethanol, water, and the like. When water is the solvent, the molecule is referred to as a “hydrate." The formation of solvates of thecompounds of the disclosure will vary depending on the compound and the solvate. In general, solvates are formed by dissolving the compound in the appropriate solvent and isolating the solvate by cooling or using an antisolvent. The solvate is typically dried or azeotroped under ambient conditions. The selection of suitable conditions to form a particular solvate can be made by a person skilled in the art.

[0252] Prodrugs of the compounds of the present application may be, for example, conventional esters formed with available hydroxy, thiol, amino or carboxyl groups. For example, available hydroxy or amino groups may be acylated using an activated acid in the presence of a base, and optionally, in inert solvent (e.g. an acid chloride in pyridine).

[0253] Isotopically-enriched compounds of the disclosure and pharmaceutically acceptable salts, solvates, and / or prodrugs thereof, can be prepared by conventional techniques well known to those skilled in the art or by processes analogous to those described in the Schemes and Examples herein using suitable isotopically-enriched reagents and / or intermediates.

[0254] Throughout the processes described herein it is to be understood that, where appropriate, suitable protecting groups will be added to and subsequently removed from, the various reactants and intermediates in a manner that will be readily understood by one skilled in the art. Conventional procedures for using such protecting groups as well as examples of suitable protecting groups are described, for example, in “Protective Groups in Organic Synthesis," T.W. Green, P.G.M. Wuts, Wiley-lnterscience, New York, (1999). It is also to be understood that a transformation of a group or substituent into another group or substituent by chemical manipulation can be conducted on any intermediate or final product on the synthetic path toward the final product, in which the possible type of transformation is limited only by inherent incompatibility of other functionalities carried by the molecule at that stage to the conditions or reagents employed in the transformation. Such inherent incompatibilities and ways to circumvent them by carrying out appropriate transformations and synthetic steps in a suitable order, will be readily understood to one skilled in the art. Examples of transformations are given herein and it is to be understood that the described transformations are not limited only to the generic groups or substituents for which the transformations are exemplified. References and descriptions of other suitable transformations are given in “Comprehensive Organic Transformations - A Guide to Functional Group Preparations” R.C. Larock, VHC Publishers, Inc. (1989). References and descriptions of other suitable reactions are described in textbooks of organic chemistry, for example, “Advanced Organic Chemistry,” March, 4th ed. McGraw Hill (1992) or, “OrganicSynthesis,” Smith, McGraw Hill, (1994). Techniques for purification of intermediates and final products include, for example, straight and reversed phase chromatography on column or rotating plate, recrystallisation, distillation and liquid-liquid or solid-liquid extraction, which will be readily understood by one skilled in the art.

[0255] Nucleophilic displacement reaction conditions comprise any known method for the reaction of a nucleophile to displace a leaving group to form a bond that is compatible with the intermediates and products shown in the above Schemes or that may be used to prepare a compound of the application. In some embodiments, such conditions comprise combining reactants in the presence of a base in a suitable solvent.

[0256] It is also to be understood that a transformation of a group or substituent into another group or substituent by chemical manipulation can be conducted on any intermediate or final product on the synthetic path toward the final product, in which the possible type of transformation is limited only by inherent incompatibility of other functionalities carried by the molecule at that stage to the conditions or reagents employed in the transformation. Such inherent incompatibilities, and ways to circumvent them by carrying out appropriate transformations and synthetic steps in a suitable order, will be readily understood to one skilled in the art. Examples of transformations are given herein, and it is to be understood that the described transformations are not limited only to the generic groups or substituents for which the transformations are exemplified. References and descriptions of other suitable transformations are given in “Comprehensive Organic Transformations - A Guide to Functional Group Preparations” R.C. Larock, VHC Publishers, Inc. (1989). References and descriptions of other suitable reactions are described in textbooks of organic chemistry, for example, “Advanced Organic Chemistry,” March, 4th ed. McGraw Hill (1992) or, "Organic Synthesis,” Smith, McGraw Hill, (1994).

[0257] Techniques for purification of intermediates and final products include, for example, straight and reversed phase chromatography on column or rotating plate, recrystallisation, distillation, and liquid-liquid or solid-liquid extraction, which will be readily understood by one skilled in the art.

[0258] The products of processes disclosed in the disclosure may be isolated according to known methods, for example, the compounds may be isolated by evaporation of the solvent, by filtration, centrifugation, chromatography, or other suitable method.

[0259] Prodrugs of the compounds of the present disclosure may be, for example, conventional esters formed with available hydroxy, thiol, amino, or carboxyl groups. For example, available hydroxy or amino groups may be acylated using an activated acid in the presence of a base, and optionally, in inert solvent (e.g., an acid chloride in pyridine).

[0260] IUPAC names were generated with MarvinSketch 24.1.3 or ChemDraw Professional 23.1.2.7.

[0261] One skilled in the art will recognize that where a reaction step of the present disclosure is carried out in a variety of solvents or solvent systems, said reaction step may also be carried out in a mixture of the suitable solvents or solvent systems.VI. Biological Testing

[0262] Compounds of the invention are tested for receptor binding to the serotonin receptors according to the procedures described below.

[0263] Human 5-Hydroxytryptamine Receptor 1A (5-HT1A) CAMP assay

[0264] Compounds of the invention are tested for potency (EC50) and efficacy (Max response) against the human 5-HT IA receptor in a cAMP assay using stably transfected CHO-K1 cells. Cells are seeded in a total volume of 20 μL into white walled, 384-well microplates and incubated at 37 °C overnight before analysis. Prior to testing, cell plating media are exchanged with 10 μL of Assay buffer (HBSS + 10 mM HEPES). Briefly, intermediate dilution of sample stocks is performed to generate 4X sample in assay buffer. 5 μL of 4X sample + 5 μL of 4X forskolin is added to cells and incubated at 37 °C for 30 minutes. Final assay vehicle concentration is 1%. The results are expressed as a percent efficacy relative to the maximum response of the control ligand (serotonin).

[0265] Human 5-Hydroxytryptamine Receptor 1A (5-HT1A) Functional FLIPR assay

[0266] Compounds of the invention are tested to assess the potential excitatory effects of compounds targeting on 5-HT1Aunder agonist mode, using FLIPR functional assay.

[0267] The results are expressed in EC50(nM) concentrations. This assay confirms compounds of the disclosure are effective agonists of the target human 5-HT1Areceptors.

[0268] Human 5-Hydroxytryptamine Receptor 1A (5-HT1A) Radioligand binding assay

[0269] Compounds of the invention are tested to evaluate the binding properties in radioligand binding assay on human 5-HT1Areceptor.

[0270] Human 5-Hydroxytryptamine Receptor 2A (5-HT2A) β-arrestins Assay

[0271] Compounds of the invention are tested for potency (EC50) and efficacy (Max response) against the human 5-HT2Areceptor in stably transfected U2OS cells in a GPCR cell based β- arrestins reporter assay. Cells are seeded in a total volume of 20 μL into white walled, 384-well microplates and incubated at 37 °C overnight before analysis. For agonist determination, cells are incubated with sample to induce response. Intermediate dilution of sample stocks is performed to generate 5X sample in assay buffer. 5 μL of 5X sample is added to cells and incubated at 37 °C for 120 minutes. Final assay vehicle concentration is 1%. The results are expressed as a percent efficacy relative to the maximum response of the control ligand (serotonin).

[0272] Human 5-Hydroxytryptamine Receptor 2A (5-HT2A) Functional FLIPR Assay

[0273] Compounds of the invention are tested to assess the potential excitatory effects of compounds targeting human 5-HT2Aunder agonist mode, using FLIPR functional assay.

[0274] The results are expressed in EC50(nM) concentrations This assay confirms compounds of the disclosure are effective agonists of the target human 5-HT2Areceptors.

[0275] Human 5-Hydroxytryptamine Receptor 2A (5-HT2A) Radioligand binding assay

[0276] Compounds of the invention are tested in the human 5-HT2A, by radioligand binding assay, to evaluate the binding properties of compounds targeting on 5-HT2A. Ketanserin, known 5-HT2Aantagonist, is used as reference compound. The results are expressed in % inhibition IC50.

[0277] Human 5-Hydroxytryptamine Receptor 2B (5-HT2B) FLIPR assay

[0278] Compounds of the invention are tested for potency (EC50) and efficacy (Max response) against the human 5-HT2Breceptor in stably transfected HEK293 cells, in a calcium mobilizationbased assay.

[0279] Cells are seeded in a total volume of 20 μL into white walled, 384-well microplates and incubated at 37 °C overnight. Prior to testing, cell plating media is exchanged with 20 μL of Dye Loading buffer (HBSS+20mM HEPES containing 1X Dye, 1X Additive A and 2.5 mM Probenecid). Plates are incubated at 37 °C for 45 mins followed by 15 mins at room temperature.

[0280] 10 μl of assay buffer (HBSS+20 mM HEPES) is added to cells. Intermediate dilution of sample stocks is performed to generate 4X sample in assay buffer. Assay plates, compound plates are loaded into FLIPR instrument. 10 μL of sample is added using FLIPR onboard roboticsafter 5 seconds of starting calcium measurement. Final assay vehicle concentration is 1%. The results are expressed as a percent efficacy relative to the maximum response of the control ligand (serotonin).

[0281] Human 5-Hydroxytryptamine Receptor 2B (5-HT2B) Positive Allosteric Modulator (PAM) Assay

[0282] Compounds of the invention are tested for potency (EC50) and efficacy (Max response) against the human 5-HT2Breceptor in stably transfected HEK293 cells, in a GPCR cell-based assay. For Positive Allosteric Modulator determination, cells are pre-incubated with sample followed by EC20 addition. Intermediate dilution of sample stocks is performed to generate 5X sample in assay buffer. 5 μL of 5X sample is added to cells and incubated at 37 °C for 10 minutes. 5 μL of agonist at 6X EC20 concentration is added, and cells are incubated at 37 °C for 120 minutes. Final assay vehicle concentration is 1%. The results are expressed as a percent efficacy relative to the maximum response of the control ligand (serotonin).

[0283] Human 5-Hydroxytryptamine Receptors 2B (5-HT2B) Radioligand binding assay

[0284] Compounds of the invention are tested in the 5-HT2B, by radioligand binding assay. Yohimbine, known 5-HT2Bantagonist, is used as reference compound. The results are expressed as % inhibition IC50.

[0285] Human 5-Hydroxytryptamine Receptors 2C (5-HT2C) FLIPR assay

[0286] Compounds of the invention are tested for potency potency (EC50) and efficacy (Max response) against the human 5-HT2Creceptor in stably transfected U2OS cells, in a calcium mobilization-based assay.

[0287] Cells are seeded in a total volume of 20 μL into white walled, 384-well microplates and incubated at 37 °C overnight. Prior to testing, cell plating media is exchanged with 20 μL of Dye Loading buffer (HBSS+20mM HEPES containing 1X Dye, 1X Additive A and 2.5 mM Probenecid). Plates are incubated at 37 °C for 45 mins followed by 15 mins at room temperature. 10 μl of assay buffer (HBSS+20 mM HEPES) is added to cells. Intermediate dilution of sample stocks is performed to generate 4X sample in assay buffer. Assay plates, compound plates are loaded into FLIPR instrument. 10 μL of sample is added using FLIPR onboard robotics after 5 seconds of starting calcium measurement. Final assay vehicle concentration is 1%. The results are expressed as a percent efficacy relative to the maximum response of the control ligand (serotonin).

[0288] Exemplary Embodiments

[0289] E1 : A compound of Formula (I) or a stereoisomer thereof:or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof, wherein:X is CR18R19, O, S(O), S(O)2, or S;R1is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C3- C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl;R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneOC1-C6alkyl, optionally substituted C3-C6cycloalkyl, optionally substituted OC3-C6cycloalkyl, optionally substituted OC1- C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1- C6alkylene(5- to 6-membered) heteroaryl, or R2and R3are linked to one another to form an O- (CH2)1-2-O- linkage;R3is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl, or Rs and R3are linked to one another to form an O-(CH2)1-2-O- linkage;R4is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl;R5is selected from H, D, halo, and optionally substituted C1-C6alkyl;R6is selected from H, D, halo, and optionally substituted C1-C6alkyl;R7is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl;Q is selected from:over a bond means that the bond is attached to a remaining portion of the compound; each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R10is independently selected from halo, optionally substituted C1-C6alkyl. optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R13is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R15is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;R16and R17are included in a structurein which R16is selected from H, D, halo,OH, and optionally substituted C1-C6alkyl, and R17is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl; ortogether form a carbonyl group having a structureR18is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl;R19is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl; m is 0, 1, or 2; n is 0, 1 , or 2; o is 0, 1 , or 2; p is 0, 1 , or 2; one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective alternative isotopes thereof; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, CH3, and OCH3, R3is selected from H and F, R4is selected from H and F, R5is H, R6is H, R7is H, Q is Q1 , and m is 0, then R9is not H;provided when X is CR18R19, R18is H, R19is selected from H and CH3, R5is CH3, R6is CH3, Q isQ2, R11is selected from H, CH3, CH2CH3, and n is 0, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R5is CH3, R6is CH3, Q is Q2, R11is CH3, n is 1 , and R10is CH3, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, CH2CH3, and OCH3, R3is selected from H and F, R4is H, R5is H, R6is H, R7is H, Q is Q2, and n is 0, then R11is not selected from H and CH3; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, Cl, Br, CH3, and OCH3, R3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, CH3, and OCH3, R5is H, R6is H, R7is H, Q is Q4, R16is H, R17is H, and p is 0, then R15is not H; and the compound of Formula (I) is not selected from the following and stereoisomers thereof:4-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1H-inden-1-yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1H-inden-1-yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

[0290] E2: The compound of E1 , wherein the compound is not selected from a partially or fully deuterated analog of the following and stereoisomers thereof:4-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzothiophene-1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2 ,3-di hyd robenzofu ran-3-y I ) py rro I id ine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihyd robenzofu ran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

[0291] E3: The compound of E1 or E2, wherein the compound is not selected from a partially or fully halogenated analog of the following and stereoisomers thereof:4-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro- 1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1 -(1 , 2, 6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

[0292] E4: The compound of any one of E1 to E3, wherein one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective bromine atoms, one or more respective chlorine atoms, and / or one or more respective fluorine atoms, and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective deuterium atoms.

[0293] E5: The compound of any one of E1 to E3, wherein one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective chlorine atoms and / or one or more respective fluorine atoms, and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective deuterium atoms.

[0294] E6: The compound of any one of E1 to E3, wherein one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective chlorine atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective deuterium atoms.

[0295] E7: The compound of any one of E1 to E3, wherein one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective fluorine atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective deuterium atoms.

[0296] E8: The compound of any one of E1 to E7, wherein R1is selected from H, D, and halo.

[0297] E9: The compound of any one of E1 to E7, wherein R1is selected from unsubstituted C1-C6alkyl, unsubstituted C3-C6cycloalkyl, unsubstituted OC1-C6alkyl, unsubstituted SC1-C6alkyl, unsubstituted OC1-C6alkyleneC(O)OH, and unsubstituted OC1-C6alkyleneOC1-C6alkyl.

[0298] E10: The compound of any one of E1 to E7, wherein R1is selected from substituted C1- C6alkyl, substituted C3-C6cycloalkyl, substituted OC1-C6alkyl, substituted SC1-C6alkyl, substituted OC1-C6alkyleneC(O)OH, and substituted OC1-C6alkyleneOC1-C6alkyl.

[0299] E11 : The compound of E10, wherein R1is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-CiOaryl, and 5- to 10-membered heteroaryl.

[0300] E12: The compound of any one of E1 to E7, wherein R1is selected from H and OCH3, wherein one or more available hydrogen atoms of R1are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0301] E13: The compound of E7, wherein R1is selected from propyl,

[0302] E14: The compound of any one of E1 to E13, wherein R2is selected from H, D, and halo.

[0303] E15: The compound of any one E1 to E13, wherein R2is selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, unsubstituted SC1-C6alkyl, unsubstituted OC1- C6alkyleneOC1-C6alkyl, unsubstituted C3-C6cycloalkyl, unsubstituted OC3-C6cycloalkyl, unsubstituted OC1-C6alkyleneC3-C6cycloalkyl, unsubstituted 5- to 6-membered heterocycloalkyl, unsubstituted O(5- to 6-membered) heterocycloalkyl, unsubstituted C6aryl, unsubstituted C1- C6alkyleneC6aryl, unsubstituted 5- to 6-membered heteroaryl, unsubstituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and unsubstituted C1-C6alkylene(5- to 6-membered) heteroaryl.

[0304] E16: The compound of any one of E1 to E13, wherein R2is selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, substituted SC1-C6alkyl, substituted OC1-C6alkyleneOC1- C6alkyl, substituted C3-C6cycloalkyl, substituted OC3-C6cycloalkyl, substituted OC1-C6alkyleneC3- C6cycloalkyl, substituted 5- to 6-membered heterocycloalkyl, substituted O(5- to 6-membered) heterocycloalkyl, substituted C6aryl, substituted C1-C6alkyleneC6aryl, substituted 5- to 6- membered heteroaryl, substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and substituted C1-C6alkylene(5- to 6-membered) heteroaryl.

[0305] E17: The compound of E16, wherein R2is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0306] E18: The compound of any one of E1 to E13, wherein R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1- C6alkyl, and optionally substituted OC1-C6alkyleneOC1-C6alkyl.

[0307] E19: The compound of E18, wherein R2is selected from H, D, F, isopropyl, OCH3, and O-propyl, wherein one or more available hydrogen atoms of R2are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0308] E20: The compound of any one of E1 to E13, wherein R2is selected from unsubstituted C3-C6cycloalkyl, unsubstituted OC3-C6cycloalkyl, and unsubstituted OC1-C6alkyleneC3- C6cycloalkyl.

[0309] E21 : The compound of any one of E1 to E13, wherein R2is selected from substituted C3-C6cycloalkyl, substituted OC3-C6cycloalkyl, and substituted OC1-C6alkyleneC3-C6cycloalkyl.

[0310] E22: The compound of E21 , wherein R2is substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and OC1-C4alkyl.

[0311] E23: The compound of any one of E1 to E13, wherein R2comprises a heterocycloalkyl moiety and is selected from optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, and optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl.

[0312] E24: The compound of E23, wherein the heterocycloalkyl moiety of R2is substituted with one or more substituents independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and OC1- C4alkyl.

[0313] E25: The compound of E23 or E24, wherein the heterocycloalkyl moiety of R2comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, and wherein the heterocycloalkyl moiety of R2optionally and additionally comprises one or two C=O groups.

[0314] E26: The compound of any one of E1 to E13, wherein R2comprises an aryl moiety and is selected from optionally substituted C6aryl and optionally substituted C1-C6alkyleneC6aryl.

[0315] E27: The compound of E26, wherein the aryl moiety of R2is substituted with one or more substituents.

[0316] E28: The compound of E27, wherein the one or more substituents of the aryl moiety of R2are independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and 0C1-C4alkyl.

[0317] E29: The compound of any one of E1 to E13, wherein R2comprises a heteroaryl moiety and is selected from optionally substituted 5- to 6-membered heteroaryl and optionally substituted C1-C6alkylene(5- to 6-membered) heteroaryl.

[0318] E30: The compound of E29, wherein the heteroaryl moiety of R2is substituted with one or more substituents.

[0319] E31 : The compound of E30, wherein the one or more substituents of the heteroaryl moiety of R2are independently selected from halo, C1-C4alkyl, SC1-C4alkyl, and OC1-C4alkyl.

[0320] E32: The compound of any one of E29 to E31, wherein the heteroaryl moiety of R2comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, and wherein the heteroaryl moiety optionally and additionally comprises one or two C=O groups.

[0321] E33: The compound of any one of E1 to E13, wherein R2comprises a member selected from

[0322] E34: The compound of any one of E1 to E13, wherein R2and R3are linked to one another to form an optionally substituted 3- to 5-membered heterocycloalkyl.

[0323] E35: The compound of E34, wherein R2and R3are linked to one another to form an optionally substituted 5-membered heterocycloalkyl.

[0324] E36: The compound of E34 or E35, wherein R2and R3are linked to one another by -O- CH2-O-.

[0325] E37: The compound of any one of E34 to E36, wherein R2and R3are linked to one another to form an unsubstituted heterocycloalkyl.

[0326] E38: The compound of E34 or E35, wherein the heterocycloalkyl comprises 1 to 3 ring heteromoieties independently selected from O, S, S(O), SO2, and N, and wherein the at least one heterocycloalkyl optionally and additionally comprises one or two C=O groups.

[0327] E39: The compound of any one of E1 to E33, wherein R3is selected from H, D, and halo.

[0328] E40: The compound of any one of E1 to E33, wherein R3is selected from optionally substituted C1-C6alkyl and optionally substituted OC1-C6alkyl.

[0329] E41 : The compound of E40, wherein R3is selected from substituted C1-C6alkyl and substituted OC1-C6alkyl.

[0330] E42: The compound of E41 , wherein R3is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0331] E43: The compound of E40, wherein R3is selected from unsubstituted C1-C6alkyl and unsubstituted OC1-C6alkyl.

[0332] E44: The compound of any one of E1 to E33, wherein R3is selected from OCH3and O- propyl, wherein one or more available hydrogen atoms of R3are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0333] E45: The compound of any one of E1 to E44, wherein R4is selected from H, D, and halo.

[0334] E46: The compound of any one of E1 to E44, wherein R4is selected from optionally substituted C1-C6alkyl and optionally substituted OC1-C6alkyl.

[0335] E47: The compound of E46, wherein R4is selected from substituted C1-C6alkyl and substituted OC1-C6alkyl.

[0336] E48: The compound of E47, wherein R4is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0337] E49: The compound of E46, wherein R4is selected from unsubstituted C1-C6alkyl and unsubstituted OC1-C6alkyl.

[0338] E50: The compound of any one of E1 to E44, wherein R4is OCH3, wherein one or more available hydrogen atoms of R4are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0339] E51 : The compound of any one of E1 to E50, wherein R5is selected from H and halo.

[0340] E52: The compound of any one of E1 to E50 wherein R5is optionally substituted C1- C6alkyl.

[0341] E53: The compound of E52, wherein R5is substituted C1-C6alkyl.

[0342] E54: The compound of E53, wherein R5is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0343] E55: The compound of E52, wherein R5is unsubstituted C1-C6alkyl.

[0344] E56: The compound of any one of E1 to E50, wherein R5is CH3, wherein one or more available hydrogen atoms of R5are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0345] E57: The compound of any one of E1 to E50, wherein R5is H not replaced with a halogen atom or an alternative isotope thereof.

[0346] E58: The compound of any one of E1 to E50, wherein R5is D.

[0347] E59: The compound of any one of E1 to E58, wherein R6is selected from H, D, and halo.

[0348] E60: The compound of any one of E1 to E58, wherein R6is optionally substituted C1- C6alkyl.

[0349] E61 : The compound of E60, wherein R6is substituted C1-C6alkyl.

[0350] E62: The compound of E61 , wherein R6is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0351] E63: The compound of E60, wherein R6is unsubstituted C1-C6alkyl.

[0352] E64: The compound of any one of E1 to E58, wherein R6is CH3, wherein one or more available hydrogen atoms of R6are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0353] E65: The compound of any one of E1 to E58, wherein R6is H not replaced with a halogen atom or an alternative isotope thereof.

[0354] EGG: The compound of any one of E1 to E58, wherein R6is D.

[0355] E67: The compound of any one of E1 to E66, wherein R7is selected from H, D, and halo.

[0356] E68: The compound of any one of E1 to E66, wherein R7is optionally substituted C1- C6alkyl.

[0357] E69: The compound of E68, wherein R7is substituted C1-C6alkyl.

[0358] E70: The compound of E69, wherein R7is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0359] E71 : The compound of E68, wherein R7is unsubstituted C1-C6alkyl.

[0360] E72: The compound of any one of E1 to E66, wherein R7is CH3, wherein one or more available hydrogen atoms of R7are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0036] ] E73: The compound of any one of E1 to E66, wherein R7is H not replaced with a halogen atom or an alternative isotope thereof.

[0362] E74: The compound of any one of E1 to E66, wherein R7is D.

[0363] E75: The compound of any one of E1 to E66, wherein R7is F.

[0364] E76: The compound of any one of E1 to E75, wherein X is CR18R19, and wherein R18is selected from H, D, and halo.

[0365] E77: The compound of any one of E1 to E75, wherein X is CR18R19, and wherein R18is selected from optionally substituted C1-C6alkyl, optionally substituted C1-C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl.

[0366] E78: The compound of E77, wherein R18is selected from substituted C1-C6alkyl, substituted C1-C6alkyleneOC1-C6alkyl, and substituted C1-C6alkyleneNHC1-C6alkyl.

[0367] E79: The compound of E78, wherein R18is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0368] E80: The compound of E77, wherein R18is selected from unsubstituted C1-C6alkyl, unsubstituted C1-C6alkyleneOC1-C6alkyl, and unsubstituted C1-C6alkyleneNHC1-C6alkyl.

[0369] E81 : The compound of any one of E76 to E80, wherein X is CR18R19, and wherein R19is selected from H, D, and halo.

[0370] E82: The compound of any one of E76 to E80, wherein X is CR18R19, and wherein R19is selected from optionally substituted C1-C6alkyl, optionally substituted C1-C6alkyleneOC1- C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl.

[0371] E83: The compound of E82, wherein R19is selected from substituted C1-C6alkyl, substituted C1-C6alkyleneOC1-C6alkyl, and substituted C1-C6alkyleneNHC1-C6alkyl.

[0372] E84: The compound of E83, wherein R19is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0373] E85: The compound of E82, wherein R19is selected from unsubstituted C1-C6alkyl, unsubstituted C1-C6alkyleneOC1-C6alkyl, and unsubstituted C1-C6alkyleneNHC1-C6alkyl.

[0374] E86: The compound of any one of E1 to E75, wherein X is CR18R19, and wherein R18and R19are each H not replaced by respective halogen atoms or respective alternative isotopes thereof.

[0375] E87: The compound of any one of E1 to E80, wherein X is CR18H, and wherein R18is not H.

[0376] E88: The compound of any one of E1 to E85, wherein X is CR18R19, and wherein neither R18nor R19is H.

[0377] E89: The compound of any one of E1 to E75, provided when X is selected from CR18R19, O, and S, Q is selected from Q1 and Q2, then R7is not OH.

[0378] E90: The compound of any one of E1 to E75, provided when X is CR18R19, Q is selected from Q1 and Q2, R18is H, and R19is H, then R7is not OH.

[0379] E91 : The compound of any one of E1 to E75, wherein X is O.

[0380] E92: The compound of any one of E1 to E75, wherein X is S.

[0381] E93: The compound of any one of E1 to E75, wherein X is S(O).

[0382] E94: The compound of any one of E1 to E75, wherein X is S(O)2.

[0383] E95: The compound of any one of E1 to E75, wherein X is selected from O, S, S(O), and S(O)2.

[0384] E96: The compound of any one of E1 to E75, provided when X is CR18R19, then Q is selected from Q3 and Q4.

[0385] E97: The compound of any one of E1 to E75, provided when X is CR18R19, R18is H, and R19is H, then Q is selected from Q3 and Q4.

[0386] E98: The compound of any one of E1 to E95, wherein Q is Q1 to provide the compound with a structure:

[0387] E99: The compound of E98, wherein m is 0.

[0388] E100: The compound of E98, wherein m is 1 or 2.

[0389] E101 : The compound of E100, wherein each R8is independently halo.

[0390] E102: The compound of E101, wherein each R8is F.

[0391] E103: The compound of E100, wherein each R8is independently selected from optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl.

[0392] E104: The compound of E103, wherein each R8is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1-C6alkyl.

[0393] E105: The compound of E104, wherein one or more of R8are substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1- C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0394] E106: The compound of E103, wherein each R8is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl.

[0395] E107: The compound of E103, wherein each R8is independently CH3, wherein one or more available hydrogen atoms of R8are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0396] E108: The compound of E100, wherein each R8is independently selected from OC1- C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R8are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0397] E109: The compound of E100, wherein each R8is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F.

[0398] E110: The compound of any one of E98 to E109, wherein R9is H not replaced with a halogen atom or an alternative isotope thereof.

[0399] E111 : The compound of any one of E98 to E109, wherein R9is selected from optionally substituted C1-C6alkyl and optionally substituted C1-C6alkyleneOC1-C6alkyl.

[0400] E112: The compound of E111 , wherein R9is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl.

[0401] E113: The compound of E112, wherein R9is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0402] E114: The compound of E111 , wherein R9is selected from unsubstituted C1-C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl.

[0403] E115: The compound of any one of E98 to E109, wherein R9is selected from H, D, and CH3, wherein one or more available hydrogen atoms of R9are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0404] E116: The compound of E115, wherein R9is selected from H, D, F, CH3, CD3, and CF3.

[0405] E117: The compound of any one of E98 to E109, wherein R9is C1-C6alkyleneOC1- C6alkyl, wherein one or more available hydrogen atoms of R9are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0406] E118: The compound of E117, wherein R9is CH2CH2OCH3.

[0407] E119: The compound of E98, wherein:X is selected from CH2, O, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R9is selected from H and CH3; m is 0; and no available hydrogen atoms are replaced by a halogen atom and no available atoms are replaced by respective alternative isotopes thereof.

[0408] E120: The compound of any one of E1 to E95, wherein Q is Q2 to provide the compound with a structure:

[0409] E121 : The compound of E120, wherein n is 0.

[0410] E122: The compound of E120, wherein n is 1 or 2.

[0411] E123: The compound of E122, wherein each R10is independently halo.

[0412] E124: The compound of E123, wherein each R10is F.

[0413] E125: The compound of E122, wherein each R10is independently selected from optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl.

[0414] E126: The compound of E125, wherein each R10is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1-C6alkyl.

[0415] E127: The compound of E126, wherein one or more of R10are substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1- C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0416] E128: The compound of E125, wherein each R10is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl.

[0417] E129: The compound of E125, wherein each R10is independently CH3, wherein one or more available hydrogen atoms of R10are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0418] E130: The compound of E125, wherein each R10is independently selected from OC1- C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R10are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0419] E131 : The compound of E125, wherein each R10is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F.

[0420] E132: The compound of any one of E120 to E131, wherein R11is H not replaced with a halogen atom or an alternative isotope thereof.

[0421] E133: The compound of any one of E120 to E131, wherein R11is selected from optionally substituted C1-C6alkyl and optionally substituted C1-C6alkyleneOC1-C6alkyl.

[0422] E134: The compound of E133, wherein R11is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl.

[0423] E135: The compound of E134, wherein R11is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0424] E136: The compound of E133, wherein R11is selected from unsubstituted C1-C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl.

[0425] E137: The compound of any one of E120 to E131 , wherein R11is selected from H, D, and CH3, wherein one or more available hydrogen atoms of R11are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0426] E138: The compound of E137, wherein R11is selected from H, D, F, CH3, CD3, and CF3.

[0427] E139: The compound of any one of E120 to E131 , wherein R11is C1-C6alkyleneOC1- C6alkyl, wherein one or more available hydrogen atoms of R11are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0428] E140: The compound of E139, wherein R11is CH2CH2OCH3.

[0429] E141 : The compound of E120, wherein:X is selected from CH2, O, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R11is selected from H and CH3; n is 0; and no available hydrogen atoms are replaced by respective halogen atoms and no available atoms are replaced by respective alternative isotopes thereof.

[0430] E142: The compound of any one of E1 to E97, wherein Q is Q3 to provide a compound with a structure:

[0431] E143: The compound of E142, wherein o is 0.

[0432] E144: The compound of E142, wherein o is 1 or 2.

[0433] E145: The compound of E144, wherein each R12is independently halo.

[0434] E146: The compound of E145, wherein each R12is F.

[0435] E147: The compound of E144, wherein each R12is independently selected from optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl.

[0436] E148: The compound of E147, wherein each R12is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1-C6alkyl.

[0437] E149: The compound of E148, wherein one or more of R12are substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1- C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0438] E150: The compound of E147, wherein each R12is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl.

[0439] E151 : The compound of E147, wherein each R12is independently CH3, wherein one or more available hydrogen atoms of R12are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0440] E152: The compound of E147, wherein each R12is independently selected from OC1- C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R12are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0441] E153: The compound of E147, wherein each R12is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F.

[0442] E154: The compound of any one of E142 to E153, wherein R13is H not replaced with a halogen atom or an alternative isotope thereof.

[0443] E155: The compound of any one of E142 to E153, wherein R13is selected from optionally substituted C1-C6alkyl and optionally substituted C1-C6alkyleneOC1-C6alkyl.

[0444] E156: The compound of E155, wherein R13is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl.

[0445] E157: The compound of E156, wherein R13is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0446] E158: The compound of E155, wherein R13is selected from unsubstituted C1-C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl.

[0447] E159: The compound of any one of E142 to E153, wherein R13is selected from H, D, and CH3, wherein one or more available hydrogen atoms of R13are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0448] E160: The compound of E159, wherein R13is selected from H, D, F, CH3, CD3, and CF3.

[0449] E161 : The compound of any one of E142 to E153, wherein R13is C1-C6alkyleneOC1- C6alkyl, wherein one or more available hydrogen atoms of R13are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0450] E162: The compound of E161 , wherein R13is CH2CH2OCH3.

[0451] E163: The compound of E142, wherein:X is selected from CH2, O, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R13is CH3;0 is 0; and no available hydrogen atoms are replaced by respective halogen atoms and no available atoms are replaced by respective alternative isotopes thereof.

[0452] E164: The compound of any one of E1 to E97, wherein Q is Q4 to provide the compound with a structure:

[0453] E165: The compound of E164, wherein X is O.

[0454] E166: The compound of E164, wherein X is S.

[0455] E167: The compound of E164, wherein X is CH2.

[0456] E168: The compound of any one of E164 to E167, wherein p is 0.

[0457] E169: The compound of any one of E164 to E167, wherein p is 1 or 2.

[0458] E170: The compound of E169, wherein each R14is independently selected from H, D, and halo.

[0459] E171 : The compound of E169, wherein each R14is independently selected from optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl.

[0460] E172: The compound of E171 , wherein each R14is independently selected from substituted C1-C6alkyl, substituted OC1-C6alkyl, and substituted SC1-C6alkyl.

[0461] E173: The compound of E172, wherein one or more R14are substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1- C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0462] E174: The compound of E171 , wherein each R14is independently selected from unsubstituted C1-C6alkyl, unsubstituted OC1-C6alkyl, and unsubstituted SC1-C6alkyl.

[0463] E175: The compound of E169, wherein each R14is independently selected from H, D, and CH3, wherein one or more available hydrogen atoms of R14are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0464] E176: The compound of E169, wherein each R14is independently selected from OC1- C6alkyl and SC1-C6alkyl, wherein one or more available hydrogen atoms of R14are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0465] E177: The compound of E169, wherein each R14is independently selected from H, D, and F.

[0466] E178: The compound of E171, wherein each R14is independently selected from CH3, CD3, CF3, OCH3, OCF3, OCH2F, OCHF2, SCF3, SCH3, SCHF2, and SCH2F.

[0467] E179: The compound of any one of E164 to E178, wherein R15is H not replaced with a halogen atom or an alternative isotope thereof.

[0468] E180: The compound of any one of E164 to E178, wherein R15is selected from optionally substituted C1-C6alkyl and optionally substituted C1-C6alkyleneOC1-C6alkyl.

[0469] E181 : The compound of E180, wherein R15is selected from substituted C1-C6alkyl and substituted C1-C6alkyleneOC1-C6alkyl.

[0470] E182: The compound of E181 , wherein R15is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0471] E183: The compound of E180, wherein R15is selected from unsubstituted C1-C6alkyl and unsubstituted C1-C6alkyleneOC1-C6alkyl.

[0472] E184: The compound of any one of E164 to E178, wherein R15is selected from H, D, and CH3, wherein one or more available hydrogen atoms of R15are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0473] E185: The compound of E 184, wherein R15is selected from H, D, F, CH3, CD3, and CF3.

[0474] E186: The compound of any one of E164 to E178, wherein R15is C1-C6alkyleneOC1- C6alkyl, wherein one or more available hydrogen atoms of R15are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0475] E187: The compound of E186, wherein R15is CH2CH2OCH3.

[0476] E188: The compound of any one of E164 to E187, wherein R16is selected from H, halo, and OH.

[0477] E189: The compound of any one of E164 to E187, wherein R16is selected from optionally substituted C1-C6alkyl.

[0478] E190: The compound of E189, wherein R16is substituted C1-C6alkyl.

[0479] E191 : The compound of E190, wherein R16is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1-C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0480] E192: The compound of E189, wherein R16is selected from unsubstituted C1-C6alkyl.

[0481] E193: The compound of any one of E164 to E187, wherein R16is independently selected from H, OH, F and CH3, wherein one or more available hydrogen atoms of R16are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0482] E194: The compound of E191 , wherein R16is H not replaced with a halogen atom or an alternative isotope thereof.

[0483] E195: The compound of E191 , wherein R16is D.

[0484] E196: The compound of any one of E164 to E195, wherein R17is selected from H, D, halo, and OH.

[0485] E197: The compound of any one of E164 to E195, wherein R17is optionally substituted C1-C6alkyl.

[0486] E198: The compound of E197, wherein R17is substituted C1-C6alkyl.

[0487] E199: The compound of E198, wherein R17is substituted with one or more substituents independently selected from OH, C(O)OH, C1-C6alkyl, C1-C6alkyleneOH, OC1-C6alkyl, SH, SC1- C6alkyl, C3-C10cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-C10aryl, and 5- to 10-membered heteroaryl.

[0488] E200: The compound of E197, wherein R17is selected from unsubstituted C1-C6alkyl.

[0489] E201 : The compound of any one of E164 to E195, wherein R17is selected from H, OH, F and CH3, wherein one or more available hydrogen atoms of R17are optionally and independently replaced with one or more respective fluorine atoms and / or one or more respective deuterium atoms.

[0490] E202: The compound of E201 , wherein R17is H not replaced with a halogen atom or an alternative isotope thereof.

[0491] E203: The compound of E201 , wherein R17is D.

[0492] E204: The compound of any one of E164 to E187, wherein R16and R17included in the structureare taken together with the bonded carbon atom to form carbonyl having a structure

[0493] E205: The compound of E164, wherein:X is selected from CH2, O, and S;R1is selected from H, D, F, OCH3, CH(CH3)2, cyclopropyl, OCH(CH3)2, OCH2CH2OCH3;R2is selected from H, D, F, CH(CH3)2, cyclopropane, optionally substituted phenyl, tetrahydropyran, optionally substituted pyridine, optionally substituted thiane, thiophene, thiazole, isothiazole, OCH3, OCF3, OCHF2, OCD3, OCH(CH3)2, OCH2-cyclopropane, O-tetrahydropyran, and O-CH2CH2OCH3; andR3is selected from H, D, OCH3, and OCH(CH3)2; orR2and R3are linked to one another by -OCH2O-;R4is selected from H, D, and OCH3;R5is H;R6is H;R7is selected from H and F;R15is selected from H, CH3, CD3, and CHCH(CH3)2; p is O;R16is selected from H and D;R17is selected from H and D; and no available hydrogen atoms are replaced by respective halogen atoms and no available atoms are replaced by respective alternative isotopes thereof.

[0494] E206: The compound of E1 , wherein:X is CH2, O, and S;R1is selected from H, D, F, OCH3, CH(CH3)2, cyclopropyl, OCH3, OCH(CH3)2, OCH2CH2OCH3;;R2is selected from is selected from H, D, F, OCH3, CH(CH3)2, cyclopropane, optionally substituted phenyl, tetrahydropyran, optionally substituted pyridine, optionally substituted thiane, thiophene, thiazole, isothiazole, OCH3, OCF3, OCHF2, OCD3, OCH(CH3)2, OCH2-cyclopropane, O- tetrahydropyran, and O-CH2CH2OCH3;R3is selected from H, D, OCH3, and OCH(CH3)2; orR2and R3are linked to one another by -OCH2O-;R4is selected from H, D, and OCH3;R5is H;R6is H;R7is H;Q is selected from Q1 , Q2, Q3, and Q4;R9is selected from H and CH3;R11is selected from H and CH3;R13is CH3;R15is selected from H, CH3, CD3, and CHCH(CH3)2;R16is selected from H and D;R17is selected from H and D; m is 0; n is O; o is O; p is 0; and no available hydrogen atoms are replaced by respective halogen atoms and no available atoms are replaced by respective alternative isotopes thereof.

[0495] E207: The compound of E1, wherein the compound is selected from Table 1 , or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0496] E208: The compound of E1, wherein the compound is selected from Table 2, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0497] E209: The compound of E1, wherein the compound is selected from Table 3, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0498] E210: The compound of E1, wherein the compound is selected from Table 4, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0499] E211 : The compound of E1, wherein the compound is selected from Table 5, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

[0500] E212: The compound of any one of E1-E57, E59-E65, E67-73, E75-E194, E196-202, and E204, wherein the compound is non-deuterated.

[0501] E213: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R5is C1-C4alkyl, R6is C1-C4alkyl, Q is Q2, and n is 0, then R7is not OH.

[0502] E214: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R1is selected from H, Br, and OCH3, R2is selected from H, F, and CH3, R3is H, R4is selected from H and F, R5is CH3, R6is CH3, Q is Q2, R11is selected from H , and n is 0, then R7is not OH.

[0503] E215: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R1is selected from H, F, Cl, Br, CH3, OCH3, OCH2CH3, OiPr, and phenyl, R2is selected fromH, F, Cl, Br, CH3, CH2CH3, OCHa, andR3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, and OCH3, R5is CH3, R6is CH3, Q is Q2, R11is selected from CH3, and n is 0, then R7is not OH.

[0504] E216: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from F and CH3, R3is H, R4is H, R5is CH3, R6is CH3, Q is Q2, R11is CH2CH3, and n is 0, then R7is not OH.

[0505] E217: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R5is C1-C6alkyl, R6is C1-C6alkyl, Q is Q2, R11is selected from H and unsubstituted C1-C6alkyl, and n is 0, then R7is not OH.

[0506] E218: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, R5is selected from halo and C1-C6alkyl, R6is selected from halo and C1-C6alkyl, Q is Q2, R11is selected from H and optionally substituted C1-C6alkyl, and n is 0, then R7is not OH.

[0507] E219: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, Q is Q1 , and m is 0, then R9is not selected from H and CH3.

[0508] E220: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, Q is Q2, and n is 0, then R11is not selected from H, CH3, CH2CH3,

[0509] E221 : The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, Q is Q3, and o is 0, then R13is not selected from H and CH3.

[0510] E222: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is H, Q is Q4, and p is 0, then R15is not H.

[0511] E223: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H, R19is CH3, Q is Q1, and m is 0, then R9is not H.

[0512] E224: The compound of any one of E1 to E7, provided when X is CR18R19, R18is H or CH3, R19is CH3, Q is Q2, and n is 0, then R11is not selected from H and CH3.

[0513] E225: The compound of any one of E1 to E7, provided when X is O, Q is Q1 , and m is 0, then R9is not H.

[0514] E226: The compound of any one of E1 to E7, provided when X is O, Q is Q2, and n is 0, then R11is not H.

[0515] E227: The compound of any one of E1 to E7, provided when X is O, Q is Q3, and o is 0, then R13is not H.

[0516] E228: The compound of any one of E1 to E7, provided when X is O, Q is Q4, and p is 0, then R15is not H.

[0517] E229: The compound of any one of E1 to E7, provided when X is S(O)2, Q is Q1 , and m is 0, then R9is not H.

[0518] E230: The compound of any one of E1 to E7, provided when X is S(O)2, Q is Q3, and o is 0, then R13is not H.

[0519] E231 : The compound of any one of E1 to E7, provided when X is S, Q is Q1, and m is 0, then R9is not H.

[0520] E232: The compound of any one of E1 to E7, provided when X is S, Q is Q2, and n is 0, then R11is not selected from H and CH3.

[0521] E233: The compound of any one of E1 to E7, provided when X is S, Q is Q3, and o is 0, then R13is not H.

[0522] E234: The compound of any one of E1 to E7, provided when X is S, Q is Q4, and p is 0, then R15is not H.

[0523] E235: A composition comprising one or more compounds of any one of E1 to E234 and a carrier.

[0524] E236: A pharmaceutical composition comprising one or more compounds of any one of E1 to E234 and a pharmaceutically acceptable carrier.

[0525] E237: A method of treating a disease, disorder, or condition, comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0526] E238: The method of E237, wherein the disease, disorder, or condition is selected from the group depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, burnout, and a combination thereof.

[0527] E239: A method of treating a depressive disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0528] E240: The method of E239, wherein the depressive disorder is selected from major depressive disorder (MDD), MDD with suicidal ideation, persistent depressive disorder, dysthymia, dysthymic disorder, seasonal affective disorder, pre-menstrual dysphoric disorder, antenatal depression, postpartum depression, postnatal depression, treatment-resistant depression, depression related to a medical condition, depression in bipolar disorder, depression related to substance use, depression related to medicine use, psychotic depression, and a combination thereof.

[0529] E241 : A method of treating a bipolar disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0530] E242: The method of E241 , wherein the bipolar disorder is selected from Bipolar I disorder, Bipolar II disorder, cyclothymia, cyclothymic disorder, bi-polar related to a medicinal condition, and a combination thereof.

[0531] E243: A method of treating an eating disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0532] E244: The method of E243, wherein the eating disorder is selected from anorexia nervosa, bulimia nervosa, avoidant restrictive food intake disorder, other specified feeding and eating disorder, pica, rumination disorder, avoidant / restrictive food intake disorder, and a combination thereof.

[0533] E245: A method of treating an impulse control disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0534] E246: The method of E245, wherein the impulse control disorder is selected from bingeeating disorder, obsessive compulsive disorder, and a combination thereof.

[0535] E247: A method of treating a personality disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0536] E248: The method of E247, wherein the personality disorder is selected from avoidant personality disorder, dependent personality disorder, borderline personality disorder, histrionic personality disorder, narcissistic personality disorder, paranoid personality disorder, and a combination thereof.

[0537] E249: A method of treating a substance use and / or behavioral addiction disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0538] E250: The method of E249, wherein the substance use and / or behavioral addiction disorder is selected from alcohol use disorder, stimulant use disorder, cannabis use disorder, opioid use disorder, tobacco use disorder, nicotine use disorder, inhalant use disorder, sedativehypnotic use disorder, anxiolytic use disorder, gambling disorder, gaming disorder, compulsive sexual behavior disorder, and a combination thereof.

[0539] E251 : A method of treating an anxiety disorder and / or a stress disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0540] E252: The method of E251, wherein the anxiety disorder and / or the stress disorder is selected from acute stress disorder, adjustment disorder in chronic illness, body dysmorphic disorder, generalized anxiety disorder, panic disorder, post-traumatic stress disorder, prolonged grief disorder, social anxiety disorder, agoraphobia, separation anxiety disorder, specific phobias, anxiety due to a medical condition, anxiety in advanced stage illness, selective mutism, and a combination thereof.

[0541] E253: A method of treating a neurodevelopmental disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0542] E254: The method of E253, wherein the neurodevelopmental disorder is selected from attention deficit hyperactivity disorder and subtypes, autism spectrum disorder, behavioral symptoms of Fragile X syndrome, and a combination thereof.

[0543] E255: A method of treating a pain disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0544] E256: The method of E255, wherein the pain disorder is selected from fibromyalgia, neuropathic pain, phantom limb pain, chronic pain, and a combination thereof.

[0545] E257: A method of treating a headache disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0546] E258: The method of E257, wherein the headache disorder is selected from cluster headaches, short-lasting unilateral neuralgiform headaches, tension-type headaches, chronic daily headache syndrome, migraine headaches, and a combination thereof.

[0547] E259: A method of treating an inflammatory disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0548] E260: The method of E259, wherein the inflammatory disorder is selected from inflammatory bowel disease, multiple sclerosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, system lupus erythematosus, systemic sclerosis, vasculitis, and a combination thereof.

[0549] E261 : A method of treating an injury-related disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0550] E262: The method of E261 , wherein the injury-related disorder is selected from cognitive and / or behavioral symptoms of TBI, functional recovery in stroke, or a combination thereof.

[0551] E263: A method of treating a neurodegenerative disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0552] E264: The method of E263, wherein the neurodegenerative disorder is selected from Alzheimer’s disease, amyotrophic lateral sclerosis (ALS), behavioral symptoms in ALS, frontotemporal dementia, Parkinson’s disease, vascular dementia, Huntington’s disease, and a combination thereof.

[0553] E265: A method of treating a functional disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0554] E266: The method of E265, wherein the functional disorder is selected from chronic fatigue syndrome, functional neurological disorder, irritable bowel syndrome, long COVID, posttreatment Lyme, and a combination thereof.

[0555] E267: A method of treating a psychotic disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0556] E268: The method of E267, wherein the psychotic disorder is selected from schizophrenia, delusional disorder, schizoaffective disorder, and a combination thereof.

[0557] E269: A method of treating a hyperkinetic movement disorder comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0558] E270: The method of E269, wherein the hyperkinetic movement disorder is selected from chorea, akathisia, asterixis, dystonia, tremor, myoclonus, tics, stereotypies, movement disorders caused by neurodegenerative disease, metabolic derangements, vascular and autoimmune disease, infections, medications, recreational drugs, and / or pregnancy, and a combination thereof.

[0559] E271 : A method of treating age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout, comprising administering a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 to a subject in need thereof.

[0560] E272: Use of a therapeutically effective amount of one or more compounds of any one of E1 to E234 and / or the composition of any one of E235 to E236 in the manufacture of a medicament for treating a depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, alcohol use disorder, post-traumatic stress disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury- related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout.

[0561] E273: Use of one or more compound of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a disease, disorder, or condition.

[0562] E274: The use of E273, wherein the disease, disorder, or condition is selected from the group depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, burnout, and a combination thereof.

[0563] E275: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a depressive disorder.

[0564] E276: The use of E275, wherein the depressive disorder is selected from major depressive disorder (MDD), MOD with suicidal ideation, persistent depressive disorder, dysthymia, dysthymic disorder, seasonal affective disorder, pre-menstrual dysphoric disorder, antenatal depression, postpartum depression, postnatal depression, treatment-resistant depression, depression related to a medical condition, depression in bipolar disorder, depression related to substance use, depression related to medicine use, psychotic depression, and a combination thereof.

[0565] E277: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a bipolar disorder.

[0566] E278: The use of E277, wherein the bipolar disorder is selected from Bipolar I disorder, Bipolar II disorder, cyclothymia, cyclothymic disorder, bi-polar related to a medicinal condition, and a combination thereof.

[0567] E279: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating an eating disorder.

[0568] E280: The use of E279, wherein the eating disorder is selected from anorexia nervosa, bulimia nervosa, avoidant restrictive food intake disorder, other specified feeding and eating disorder, pica, rumination disorder, avoidant / restrictive food intake disorder, and a combination thereof.

[0569] E281 : Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating an impulse control disorder.

[0570] E282: The use of E281 , wherein the impulse control disorder is selected from bingeeating disorder, obsessive compulsive disorder, and a combination thereof.

[0571] E283: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a personality disorder.

[0572] E284: The use of E283, wherein the personality disorder is selected from avoidant personality disorder, dependent personality disorder, borderline personality disorder, histrionic personality disorder, narcissistic personality disorder, paranoid personality disorder, and a combination thereof.

[0573] E285: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a substance a\buse and / or behavioral addiction disorder.

[0574] E286: The use of E285, wherein the substance abuse and / or behavioral addiction disorder is selected from alcohol use disorder, stimulant use disorder, cannabis use disorder, opioid use disorder, tobacco use disorder, nicotine use disorder, inhalant use disorder, sedativehypnotic use disorder, anxiolytic use disorder, gambling disorder, gaming disorder, compulsive sexual behavior disorder, and a combination thereof.

[0575] E287: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating anxiety disorder and / or a stress disorder.

[0576] E288: The use of E287, wherein the anxiety disorder and / or the stress disorder is selected from acute stress disorder, adjustment disorder in chronic illness, body dysmorphic disorder, generalized anxiety disorder, panic disorder, post-traumatic stress disorder, prolonged grief disorder, social anxiety disorder, agoraphobia, separation anxiety disorder, specific phobias, anxiety due to a medical condition, anxiety in advanced stage illness, selective mutism, and a combination thereof.

[0577] E289: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a neurodevelopmental disorder.

[0578] E290: The use of E289, wherein the neurodevelopmental disorder is selected from attention deficit hyperactivity disorder and subtypes, autism spectrum disorder, behavioral symptoms of Fragile X syndrome, and a combination thereof.

[0579] E291 : Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a pain disorder.

[0580] E292: The use of E291, wherein the pain disorder is selected from fibromyalgia, neuropathic pain, phantom limb pain, chronic pain, and a combination thereof.

[0581] E293: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a headache disorder.

[0582] E294: The use of E293, wherein the headache disorder is selected from cluster headaches, short-lasting unilateral neuralgiform headaches, tension-type headaches, chronic daily headache syndrome, migraine headaches, and a combination thereof.

[0583] E295: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating an inflammatory disorder.

[0584] E296: The use of E295, wherein the inflammatory disorder is selected from inflammatory bowel disease, multiple sclerosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, system lupus erythematosus, systemic sclerosis, vasculitis, and a combination thereof.

[0585] E297: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating an injury-related disorder.

[0586] E298: The use of E297, wherein the injury-related disorder is selected from cognitive and / or behavioral symptoms of TBI, functional recovery in stroke, or a combination thereof.

[0587] E299: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a neurodegenerative disorder.

[0588] E300: The use of E299, wherein the neurodegenerative disorder is selected from Alzheimer’s disease, amyotrophic lateral sclerosis (ALS), behavioral symptoms in ALS, frontotemporal dementia, Parkinson's disease, vascular dementia, Huntington's disease, and a combination thereof.

[0589] E301 : Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 making a medicament for treating a functional disorder.

[0590] E302: The use of E301 , wherein the functional disorder is selected from chronic fatigue syndrome, functional neurological disorder, irritable bowel syndrome, long COVID, post-treatment Lyme, and a combination thereof.

[0591] E303: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a psychotic disorder.

[0592] E304: The use of E303, wherein the psychotic disorder is selected from schizophrenia, delusional disorder, schizoaffective disorder, and a combination thereof.

[0593] E305: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating a hyperkinetic movement disorder.

[0594] E306: The use of E305, wherein the hyperkinetic movement disorder is selected from chorea, akathisia, asterixis, dystonia, tremor, myoclonus, tics, stereotypies, movement disorders caused by neurodegenerative disease, metabolic derangements, vascular and autoimmune disease, infections, medications, recreational drugs, and / or pregnancy, and a combination thereof.

[0595] E307: Use of one or more compounds of any one of E1 to E234 and / or a composition of any one of E235 to E236 for making a medicament for treating age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout.

[0596] While the present disclosure has been described with reference to examples, it is to be understood that the scope of the claims should not be limited by the embodiments set forth in the examples but should be given the broadest interpretation consistent with the description as a whole.

Claims

1. WHAT IS CLAIMED IS:

1. A compound of Formula (I) or a stereoisomer thereof:or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof, wherein:X is CR18R19, O, S(O), S(O)2, or S;R1is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C3. C6cycloalkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneC(O)OH, and optionally substituted OC1-C6alkyleneOC1-C6alkyl;R2is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, optionally substituted SC1-C6alkyl, optionally substituted OC1-C6alkyleneOC1-C6alkyl, optionally substituted C3.C6cycloalkyl, optionally substituted OC3-C6cycloalkyl, optionally substituted OC1- C6alkyleneC3-C6cycloalkyl, optionally substituted 5- to 6-membered heterocycloalkyl, optionally substituted O(5- to 6-membered) heterocycloalkyl, optionally substituted C6aryl, optionally substituted C1-C6alkyleneC6aryl, optionally substituted 5- to 6-membered heteroaryl, optionally substituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and optionally substituted C1- C6alkylene(5- to 6-membered) heteroaryl, or R2and R3are linked to one another to form an O- (CH2)1-2-O- linkage;R3is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl, or R3and R2are linked to one another to form the O-(CH2)1-2-O- linkage;R4is selected from H, D, halo, optionally substituted C1-C6alkyl, and optionally substituted OC1- C6alkyl;R5is selected from H, D, halo, and optionally substituted C1-C6alkyl;R6is selected from H, D, halo, and optionally substituted C1-C6alkyl;R7is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl;Q is selected from:over a bond means that the bond is attached to a remaining portion of the compound; each R8is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R9is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R10is independently selected from halo, optionally substituted C1-C6alkyl. optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R11is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl; each R12is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R13is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;each R14is independently selected from halo, optionally substituted C1-C6alkyl, optionally substituted OC1-C6alkyl, and optionally substituted SC1-C6alkyl;R15is selected from H, D, optionally substituted C1-C6alkyl, and optionally substituted C1- C6alkyleneOC1-C6alkyl;R16and R17are included in a structurein which R16is selected from H, D, halo,OH, and optionally substituted C1-C6alkyl, and R17is selected from H, D, halo, OH, and optionally substituted C1-C6alkyl; ortogether form a carbonyl group having a structureR18is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl;R19is selected from H, D, halo, optionally substituted C1-C6alkyl, optionally substituted C1- C6alkyleneOC1-C6alkyl, and optionally substituted C1-C6alkyleneNHC1-C6alkyl; m is 0, 1, or 2; n is 0, 1 , or 2; o is 0, 1 , or 2; p is 0, 1 , or 2; one or more available hydrogen atoms of R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R14, R16, R17, R18, and R19and one or more available hydrogen atoms of the optionally substituted C1-C6alkyl and the optionally substituted C1-C6alkyleneOC1-C6alkyl of R9, R11, R13, and R15are optionally and independently replaced with one or more respective halogen atoms and / or one or more available atoms of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, and R19are optionally and independently replaced with one or more respective alternative isotopes thereof; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, CH3, and OCH3, R3is selected from H and F, R4is selected from H and F, R5is H, R6is H, R7is H, Q is Q1 , and m is 0, then R9is not H;provided when X is CR18R19, R18is H, R19is selected from H and CH3, R5is CH3, R6is CH3, Q isQ2, R11is selected from H, CH3, CH2CH3,and n is 0, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R5is CH3, R6is CH3, Q is Q2, R11is CH3, n is 1 , and R10is CH3, then R7is not OH; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, CH2CH3, and OCH3, R3is selected from H and F, R4is H, R5is H, R6is H, R7is H, Q is Q2, and n is 0, then R11is not selected from H and CH3; provided when X is CR18R19, R18is H, R19is H, R1is H, R2is selected from H, F, Cl, Br, CH3, and OCH3, R3is selected from H, F, Cl, Br, CH3, and OCH3, R4is selected from H, F, Cl, Br, CH3, and OCH3, R5is H, R6is H, R7is H, Q is Q4, R16is H, R17is H, and p is 0, then R15is not H; and the compound of Formula (I) is not selected from the following and stereoisomers thereof:4-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

2. The compound of claim 1 , wherein the compound is not selected from a partially or fully deuterated analog of the following:4-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2 ,3-di hyd robenzofu ran-3-y I ) py rro I id ine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihyd robenzofu ran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

3. The compound of claim 1 or claim 2, wherein the compound is not selected from a partially or fully halogenated analog of the following:4-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;3-(pyrrolidin-3-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-(piperidin-3-yl)-2,3-dihydro-1 λ6-benzoth iophene- 1 ,1 -dione;3-(2,3-dihydro-1 H-inden-1 -yl)piperidine;3-(2,3-dihydro-1-benzothiophen-3-yl)pyrrolidine;3-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(2,3-dihydro-1-benzothiophen-3-yl)piperidine;3-(2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;2-[(2,3-dihydro- 1 H-inden-1 -yl)methyl]pyrrolidine;6,6-dimethyl-5-(1-methylpiperidin-4-yl)-6,7-dihydro-5H-indeno[5,6-d][1 ,3]dioxol-5-ol;2-methyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)pyrrolidine;4-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(piperidin-4-yl)-2,3-dihydrobenzofuran-5-ol;3-(2-methyl-2,3-dihydrobenzofuran-3-yl)piperidine;3-(6-fluoro-2,3-dihydrobenzofuran-3-yl)piperidine;2,2,5-trimethyl-3-(1-methylpiperidin-4-yl)-2,3-dihydrobenzo[b]thiophen-3-ol;4-(2,3-dihydrobenzo[b]thiophen-3-yl)-1-methylpiperidine;3-(3-methyl-2,3-dihydro-1 H-inden-1 -yl)pyrrolidine;4-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-1-yl)piperidine;2,2,6-trimethyl-1-(1-methylpyrrolidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,6-trimethyl-1-(1-methylpiperidin-3-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2,3,6-tetramethyl-1-(1,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;2,2,6-trimethyl-1-(1 ,2,6-trimethylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1-ol;2-(2-hydroxyethyl)-2,6-dimethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol;2,2-diethyl-1-(1-methylpiperidin-4-yl)-2,3-dihydro-1H-inden-1-ol;1-(1-methylpiperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol; and1-(piperidin-4-yl)-2,3-dihydro-1 H-inden-1 -ol.

4. The compound of any one of claims 1-3, wherein R2is selected from unsubstituted C1- C6alkyl, unsubstituted OC1-C6alkyl, unsubstituted SC1-C6alkyl, unsubstituted OC1-C6alkyleneOC1- C6alkyl, unsubstituted C3-C6cycloalkyl, unsubstituted OC3-C6cycloalkyl, unsubstituted OC1- C6alkyleneC3-C6cycloalkyl, unsubstituted 5- to 6-membered heterocycloalkyl, unsubstituted O(5- to 6-membered) heterocycloalkyl, unsubstituted C6aryl, unsubstituted C1-C6alkyleneC6aryl, unsubstituted 5- to 6-membered heteroaryl, unsubstituted C1-C6alkylene(5- to 6-membered) heterocycloalkyl, and unsubstituted C1-C6alkylene(5- to 6-membered) heteroaryl.

5. The compound of any one of claims 1 to 3, wherein R2comprises a member selected from6. The compound of any one of claims 1 to 3, wherein R2and R3are linked to one another with the -O-CH2-O-.

7. The compound of any one of claims 1 to 6, wherein R3is selected from optionally substituted C1-C6alkyl and optionally substituted OC1-C6alkyl.

8. The compound of any one of claims 1 to 7, wherein R4is selected from optionally substituted C1-C6alkyl and optionally substituted OC1-C6alkyl.

9. The compound of any one of claims 1 to 8, wherein R5is optionally substituted C1-C6alkyl.

10. The compound of any one of claims 1 to 9, wherein X is selected from CR18R19, O, and S, wherein Q is selected from Q1 and Q2, and wherein R7is not OH.

11. The compound of any one of claims 1 to 9, wherein X is O.

12. The compound of any one of claims 1 to 9, wherein X is S.

13. The compound of any one of claims 1 to 9, wherein X is S(O).

14. The compound of any one of claims 1 to 9, wherein X is S(O)2.

15. The compound of claim 1 , wherein Q is Q1 and the compound has the structure:and wherein:X is selected from CH2, O, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R9is selected from H and CH3; m is 0; and no available hydrogen atoms are replaced by a halogen atom and no available atom is replaced by an isotope thereof.

16. The compound of claim 1 , wherein Q is Q2 and the compound has the structure:; and wherein:X is selected from CH2, 0, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R11is selected from H and CH3; n is 0; and no available hydrogen atoms are replaced by a halogen atom and no available atom is replaced by an isotope thereof.

17. The compound of claim 1 , wherein Q is Q3 and the compound has the structure:and wherein:X is selected from CH2, O, and S;R1is selected from H and OCH3;R2is selected from H and OCH3,R3is selected from H and OCH3,R4is H;R5is H;R6is H;R7is H;R13is CH3;0 is 0; and no available hydrogen atoms are replaced by a halogen atom and no available atom is replaced by an isotope thereof.

18. The compound of claim 1 , wherein Q is Q4 and the compound has the structure:and wherein:X is selected from CH2, O, and S;R1is selected from H, D, F, OCH3, CH(CH3)2, cyclopropyl, OCH(CH3)2, OCH2CH2OCH3;R2is selected from H, D, F, CH(CH3)2, cyclopropane, optionally substituted phenyl, tetrahydropyran, optionally substituted pyridine, optionally substituted thiane, thiophene, thiazole, isothiazole, OCH3, OCF3, OCHF2, OCD3, OCH(CH3)2, OCH2-cyclopropane, O-tetrahydropyran, and O-CH2CH2OCH3; andR3is selected from H, D, OCH3, and OCH(CH3)2; orR2and R3are linked to one another by -OCH2O-;R4is selected from H, D, and OCH3;R5is H;R6is H;R7is selected from H and F;R15is selected from H, CH3, CD3, and CHCH(CH3)2; p is 0;R16is selected from H and D;R17is selected from H and D; and no available hydrogen atoms are replaced by a halogen atom and no available atom is replaced by an isotope thereof.

19. The compound of claim 1 , wherein:X is CH2, O, and S;R1is selected from H, D, F, OCH3, CH(CH3)2, cyclopropyl, OCH3, OCH(CH3)2, OCH2CH2OCH3;;R2is selected from is selected from H, D, F, OCH3, CH(CH3)2, cyclopropane, optionally substituted phenyl, tetrahydropyran, optionally substituted pyridine, optionally substituted thiane, thiophene, thiazole, isothiazole, OCH3, OCF3, OCHF2, OCD3, OCH(CH3)2, OCH2-cyclopropane, O- tetrahydropyran, and O-CH2CH2OCH3;R3is selected from H, D, OCH3, and OCH(CH3)2; orR2and R3are linked to one another by -OCH2O-;R4is selected from H, D, and OCH3;R5is H;R6is H;R7is H;Q is selected from Q1 , Q2, Q3, and Q4;R9is selected from H and CH3;R11is selected from H and CH3;R13is CH3;R15is selected from H, CH3, CD3, and CHCH(CH3)2;R16is selected from H and D;R17is selected from H and D; m is 0; n is O; o is 0;p is 0; and no available hydrogen atoms are replaced by a halogen atom and no available atom is replaced by an isotope thereof.

20. The compound of claim 1 , wherein the compound is selected from:(2R)-2-[(2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2R)-2-{[(3S)-2,3-dihydro-1-benzofuran-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[(3R)-2,3-dihydro-1-benzofuran-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-[(5-fluoro-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-{[(3S)-5-fluoro-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;;(2R)-2-{[(3R)-5-fluoro-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine(2S)-2-[(2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-methylpyrrolidine;(2R)-2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]-1-(2H3)methylpyrrolidine;(2S)-2-[(2,3-dihydro-1-benzofuran-3-yl)methyl]-1-(2H3)methylpyrrolidine;2R)-2-{[2,3-dihydro(4,5,6,7-2H4)-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[2,3-dihydro(4,5,6,7-2H4)-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-2-[(2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-methylpyrrolidine;(2S)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-{[(3S)-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-(2H3)methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2S)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2R)-1-methyl-2-{[5-(trifluoromethoxy)-2,3-dihydro-1-benzofuran-3-yl](2H2)methyl}pyrrolidine;(2R)-2-{[5-(difluoromethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpynrolidine;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[5-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[5-(oxan-4-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[5-(oxan-4-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)pyridine;2-fluoro-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)pyridine;2-methoxy-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)pyridine;(2R)-2-{[5-(4-fluorophenyl)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[5-(thian-4-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)-1λ6-thiane-1,1 -dione;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)-1λ4-thian-1-one;(2R)-1-methyl-2-{[5-(propan-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(propan-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(propan-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 -benzofuran-5-yl)-1 ,2-thiazole;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzofuran-5-yl)-1 ,3-thiazole;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzofuran-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzofuran-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]pyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-(2H3)methylpyrrolidine;(2R)-1-methyl-2-[(4,5,6-trimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;(2R)-2-[(4,5-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-1 -methyl-2-({4,6,10-trioxatricyclo[7.3.0.03,7]dodeca-1 ,3(7),8-trien-12-yl}methyl)pyrrolidine;(2R)-1-(2H3)methyl-2-({4,6,10-trioxatricyclo[7.3.0.03,7]dodeca-1,3(7),8-trien-12- yl}methyl)pyrrolidine;(2R)-1 -methyl-2-({4,6,10-trioxatricyclo[7.3.0.3,7]dodeca-1 ,3(7),8-trien-12- yl}(2H2)methyl)pyrrolidine;(2R)-1-(2H3)methyl-2-({4,6,10-trioxatricyclo[7.3.0.03,7]dodeca-1,3(7),8-trien-12- yl}(2H2)methyl)pyrrolidine;(2R)-2-[(5,6,7-trimethoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]pyrrolidine;(2R)-1-methyl-2-[(5,6,7-trimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;(2R)-1-methyl-2-[(4,5,6-trimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;(2R)-2-[(4,5-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5,7-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(4-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-{[(3S)-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-[(7-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(4,7-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(6,7-dimethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2R)-1-methyl-2-[(4,5,6,7-tetramethoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine;(2S)-2-[(3-fluoro-5-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]-1-methylpyrrolidine;(2S)-2-{[(3R)-3-fluoro-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2S)-2-{[(3S)-3-fluoro-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;3-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1-methylpyrrolidine;3-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)pyrrolidine;4-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)piperidine;4-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;3-(4-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1-methylpyrrolidine;3-(6-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1-methylpyrrolidine;4-(4-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;4-(6-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;3-(6-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;3-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;3-(4-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine;(2R)-2-{[(3S)-5-fluoro-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-5-fluoro-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3S)-5-cyclopropyl-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-5-cyclopropyl-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[(3S)-4-(propan-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-4-(propan-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-2-{[(3S)-4-cyclopropyl-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-4-cyclopropyl-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(thiophen-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(thiophen-2-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(thiophen-3-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(thiophen-3-yl)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(oxan-4-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(oxan-4-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-4-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-4-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-6-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-6-(propan-2-yloxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}pyrrolidine;(2R)-2-{[(3R)-5-(2-methoxyethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(3S)-5-(2-methoxyethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(3R)-4-(2-methoxyethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(3S)-4-(2-methoxyethoxy)-2,3-dihydro-1-benzofuran-3-yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(3R)-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(3S)-4-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(3R)-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(3S)-5-methoxy-2,3-dihydro-1-benzofuran-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)methyl]pyrrolidine; and4-(5-methoxy-2,3-dihydro-1-benzofuran-3-yl)-1 -methylpiperidine, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

21. The compound of claim 1 , wherein the compound is selected from:(2R)-2-[(2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methylpyrrolidine;(2R)-2-{[( 1 S)-2,3-dihydro-1 H-inden-1 -yl](2H2)methyl}-1 -(2H3)methylpyrrolidine;(2R)-2-{[(1 R)-2,3-dihydro-1 H-inden-1 -yl](2H2)methyl}-1 -(2H3)methylpyrrolidine;(2R)-2-[(6-fluoro-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-{[(1 S)-6-fluoro-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[( 1 R)-6-fluoro-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2S)-2-[(2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -methylpyrrolidine;(2R)-2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -(2H3)methylpyrrolidine;(2S)-2-[(2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -(2H3)methyl pyrrolidine;(2R)-2-{[2,3-dihydro(4,5,6,7-2H4)-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[2, 3-dihydro(4, 5, 6, 7-2H4)-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-2-[(2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -methylpyrrolidine;(2S)-2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-{[(1 S)-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1 R)-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -(2H3)methylpyrrolidine;(2R)-2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methylpyrrolidine;(2S)-2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methylpyrrolidine;2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methyl pyrrolidine;(2R)-1 -methyl-2-{[6-(trifluoromethoxy)-2,3-dihydro-1 H-inden-1 -yl](2H2)methyl}pyrrolidine;(2R)-2-{[6-(difluoromethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[6-(2H3)methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}- 1 -(2H3)methylpyrrolidine;(2R)-2-{[6-(2H3)methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}- 1 -methylpyrrolidine;(2R)-1-methyl-2-{[6-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[6-(oxan-4-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[6-(oxan-4-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 H-inden-5-yl)pyridine;2-fluoro-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 H-inden-5-yl)pyridine;2-methoxy-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1H-inden-5-yl)pyridine;(2R)-2-{[6-(4-fluorophenyl)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-1-methyl-2-{[6-(thian-4-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 H-inden-5-yl)-1λ6-thiane-1 ,1 -dione;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1H-inden-5-yl)-1M-thian-1-one;(2R)-1-methyl-2-{[6-(propan-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-6-(propan-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 R)-6-(propan-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;4-(3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 H-inden-5-yl)-1 ,2-thiazole;4-(3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 H-inden-5-yl)-1 ,3-thiazole;(2R)-2-{[6-(2H3)methoxy-2,3-dihydro-1 H-inden-1 -yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[6-(cyclopropylmethoxy)-2,3-dihydro-1 H-inden-1 -yl](2H2)methyl}-1 - (2H3)methylpyrrolidine;(2R)-2-{[6-(cyclopropylmethoxy)-2,3-dihydro-1H-inden-1-yl]methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[6-(cyclopropylmethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]pyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1-(2H3)methylpyrrolidine;(2R)-1 -methyl-2-[(5, 6, 7-trimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl] pyrrolidine;(2R)-2-[(6,7-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-({2H,5H,6H,7H-indeno[5,6-d][1 ,3]dioxol-5-yl}methyl)-1-methylpyrrolidine;(2R)-2-({2H,5H,6H,7H-indeno[5,6-d][1 ,3]dioxol-5-yl}methyl)-1-(2H3)methylpyrrolidine;(2R)-2-({2H,5H,6H,7H-indeno[5,6-d][1 ,3]dioxol-5-yl}(2H2)methyl)-1-methylpyrrolidine;(2R)-2-({2H,5H,6H,7H-indeno[5,6-d][1 ,3]dioxol-5-yl}(2H2)methyl)-1-(2H3)methylpyrrolidine;(2R)-2-[(4,5,6-trimethoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]pyrrolidine;(2R)-1-methyl-2-[(4,5,6-trimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;(2R)-1 -methyl-2-[(5, 6, 7-trimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl] pyrrolidine;(2R)-2-[(6,7-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(4,6-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(7-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-{[(1 S)-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(1 R)-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-[(4-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(4,7-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-2-[(4,5-dimethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2R)-1 -methyl-2-[(4, 5, 6, 7-tetramethoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]pyrrolidine;(2S)-2-[(1-fluoro-6-methoxy-2,3-dihydro-1 H-inden-1 -yl)methyl]-1 -methylpyrrolidine;(2S)-2-{[(1 R)-1-fluoro-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine(2S)-2-{[(1S)-1-fluoro-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;;3-(6-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpyrrolidine;2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methylpyrrolidine;2-[(6-methoxy-2,3-dihydro-1 H-inden-1 -yl)(2H2)methyl]-1 -(2H3)methylpyrrolidine;3-(7-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpyrrolidine;3-(5-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpyrrolidine;4-(7-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpiperidine;4-(5-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpiperidine;3-(5-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpiperidine;3-(6-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpiperidine;3-(7-methoxy-2,3-dihydro-1 H-inden-1-yl)-1 -methylpiperidine;(2R)-2-{[( 1 S)-6-fluoro-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1 R)-6-fluoro-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[( 1 S)-6-cyclopropyl-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[( 1 R)-6-cyclopropyl-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-1-methyl-2-{[(1S)-7-(propan-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1R)-7-(propan-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-2-{[(1 S)-7-cyclopropyl-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1 R)-7-cyclopropyl-2,3-dihydro-1 H-inden-1-yl]methyl}-1-methylpyrrolidine;(2R)-1 -methyl-2-{[(1 R)-6-(thiophen-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 S)-6-(thiophen-2-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 R)-6-(thiophen-3-yl)-2,3-dihydro-1 H-inden-1-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-6-(thiophen-3-yl)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 R)-6-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-6-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1 R)-6-(oxan-4-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-6-(oxan-4-yloxy)-2,3-dihydro-1 H-inden-1-yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 R)-7-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-7-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1 -methyl-2-{[(1 R)-5-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(1S)-5-(propan-2-yloxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}pyrrolidine;(2R)-2-{[(1 R)-6-(2-methoxyethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1S)-6-(2-methoxyethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1 R)-7-(2-methoxyethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1S)-7-(2-methoxyethoxy)-2,3-dihydro-1 H-inden-1 -yl]methyl}-1 -methylpyrrolidine;(2R)-2-{[(1 R)-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}- 1 -(propan-2-yl)pyrrolidine;(2R)-2-{[(1S)-7-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(1 R)-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}- 1 -(propan-2-yl)pyrrolidine;(2R)-2-{[(1S)-6-methoxy-2,3-dihydro-1 H-inden-1 -yl]methyl}-1-(propan-2-yl)pyrrolidine; or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

22. The compound of claim 1 , wherein the compound is selected from:(2R)-2-[(2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2R)-2-{[(3S)-2,3-dihydro-1 -benzothiophen-3-yl](2H2)methyl}-1 -(2H3)methylpyrrolidine;(2R)-2-{[(3R)-2,3-dihydro-1 -benzothiophen-3-yl](2H2)methyl}-1-(2H3)methyl pyrrolidine;(2R)-2-{[(3R)-5-fluoro-2,3-dihydro-1 -benzothiophen-3-yl](2H2)methyl}-1-methylpyrrolidine;(2R)-2-[(5-fluoro-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1 -methylpyrrolidine;(2R)-2-{[(3S)-5-fluoro-2,3-dihydro-1-benzothiophen-3-yl](2H2)methyl}-1-methylpyrrolidine;(2S)-2-[(5-fluoro-2,3-dihydro-1 -benzothiophen-3-yl)(2H2)methyl]-1 -methyl pyrrolidine;(2S)-2-[(2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1 -methylpyrrolidine;(2R)-2-[(2,3-dihydro-1 -benzothiophen-3-yl)(2H2)methyl]-1-methylpyrrolidine;(2R)-2-[(2,3-dihydro-1 -benzothiophen-3-yl)methyl]-1 -(2H3)methyl pyrrolidine;(2S)-2-[(2,3-dihydro-1-benzothiophen-3-yl)methyl]-1 -(2H3)methylpyrrolidine;(2R)-2-{[2,3-dihydro(4,5,6,7-2H4)-1 -benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[2,3-dihydro(4,5,6,7-2H4)-1 -benzothiophen-3-yl]methyl}pyrrolidine;(2R)-2-[(2,3-dihydro-1 -benzothiophen-3-yl)(2H2)methyl]pyrrolidine;(2S)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1 -methylpyrrolidine;(2S)-2-[(5-fluoro-2,3-dihydro-1 -benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5-fluoro-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-{[(3S)-5-fluoro-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1 -methyl pyrrolidine;(2R)-2-{[(3R)-5-fluoro-2,3-dihydro-1-benzothiophen-3-yl]methyl)-1-methylpyrrolidine;(2R)-2-{[(3S)-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-(2H3)methyl pyrrolidine;(2S)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-(2H3)methylpyrrolidine;(2R)-1-methyl-2-{[5-(trifluoromethoxy)-2,3-dihydro-1-benzothiophen-3- yl](2H2)methyl}pyrrolidine;(2R)-1-methyl-2-{[5-(trifluoromethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-2-{[5-(difluoromethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[5-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[5-(oxan-4-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)pyridine;2-fluoro-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)pyridine;2-methoxy-4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5- yl)pyridine;(2R)-2-{[5-(4-fluorophenyl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[5-(thian-4-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)-1λ4-thian-1-one;4-(3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)-1λ6-thiane-1,1- dione;(2R)-1-methyl-2-{[5-(propan-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(propan-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(propan-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;4-(3-{[(2R)-1,2-dimethylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)-1,2-thiazole;4-(3-{[(2R)-1,2-dimethylpyrrolidin-2-yl]methyl}-2,3-dihydro-1-benzothiophen-5-yl)-1,3-thiazole;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzothiophen-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzothiophen-3-yl](2H2)methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(cyclopropylmethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1-methylpyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]pyrrolidine;(2R)-2-[(5,6-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-(2H3)methylpyrrolidine;(2R)-1-methyl-2-[(4,5,6-trimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-2-[(4,5-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-({4,6-dioxa-10-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8-trien-12-yl}methyl)-1- methyl pyrrolidine;(2R)-2-({4,6-dioxa-10-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8-trien-12-yl}methyl)-1- (2H3)methylpyrrolidine;(2R)-2-({4,6-dioxa-10-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8-trien-12-yl}(2H2)methyl)-1- methylpyrrolidine;(2R)-2-({4,6-dioxa-10-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8-trien-12-yl}(2H2)methyl)-1- (2H3)methylpyrrolidine;(2R)-2-[(5,6,7-trimethoxy-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]pyrrolidine;(2R)-1-methyl-2-[(5,6,7-trimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-2-[(5,6,7-trimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-1-methyl-2-[(4,5,6-trimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-2-[(4,5-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(5,7-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-2-[(5,7-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(4-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-{[(3S)-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-[(7-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(4,7-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-2-[(6,7-dimethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2R)-1-methyl-2-[(4,5,6,7-tetramethoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2S)-2-[(3-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]-1-methylpyrrolidine;(2S)-2-{[(3R)-3-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-3-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2S)-2-{[(3S)-3-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine(2R)-2-{[(3S)-3-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;3-(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1-methylpyrrolidine;;4-(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)piperidine;4-(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1 -methylpiperidine;3-(4-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1-methylpyrrolidine;3-(6-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1-methylpyrrolidine;4-(6-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1 -methylpiperidine;3-(6-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1 -methylpiperidine;3-(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1 -methylpiperidine;3-(4-methoxy-2,3-dihydro-1-benzothiophen-3-yl)-1 -methylpiperidine;(2R)-2-{[(3R)-5-fluoro-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3S)-5-fluoro-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3S)-4-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-4-fluoro-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3R)-5-cyclopropyl-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3S)-5-cyclopropyl-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[(3S)-4-(propan-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-4-(propan-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-2-{[(3R)-4-cyclopropyl-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-2-{[(3S)-4-cyclopropyl-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(thiophen-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(thiophen-2-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(thiophen-3-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(thiophen-3-yl)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-5-(oxan-4-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-5-(oxan-4-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-4-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pynrolidine;(2R)-1-methyl-2-{[(3S)-4-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3S)-6-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-1-methyl-2-{[(3R)-6-(propan-2-yloxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}pyrrolidine;(2R)-2-{[(3R)-5-(2-methoxyethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1- methylpyrrolidine;(2R)-2-{[(3S)-5-(2-methoxyethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1- methylpyrrolidine;(2R)-2-{[(3S)-4-(2-methoxyethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1- methylpyrrolidine;(2R)-2-{[(3R)-4-(2-methoxyethoxy)-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1- methylpyrrolidine;(2R)-2-{[(3R)-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(3S)-4-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-(propan-2-yl)pyrrolidine;(2R)-2-{[(3S)-5-methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-(propan-2-yl)pyrrolidine; and(2R)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)methyl]pyrrolidine;(2R)-2-{[(3R)-5-fluoro-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-methylpyrrolidine;(2S)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2R)-2-[(5-methoxy-2,3-dihydro-1-benzothiophen-3-yl)(2H2)methyl]-1-(2H3)methylpyrrolidine;(2R)-2-{[5-(2H3)methoxy-2,3-dihydro-1-benzothiophen-3-yl]methyl}-1-(2H3)methylpyrrolidine; and(2R)-1 -methyl-2-{[5-(oxan-4-yl)-2,3-dihydro-1 -benzothiophen-3-yl]methyl}pyrrolidine, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

23. The compound of claim 1 , wherein the compound is selected from:3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;5-fluoro-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;(3S)-5-fluoro-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;(3R)-5-fluoro-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;3-{[(2S)-1-methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;3-{[(2S)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro(4,5,6,7-2H4)-1λ4-benzothiophen-1-one;3-{[(2R)-pyrrolidin-2-yl]methyl}-2,3-dihydro(4,5,6,7-2H4)-1λ4-benzothiophen-1 -one;3-{[(2R)-1-methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;5-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;(3S)-5-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;(3R)-5-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;5-methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;5-methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen- 1 -one;5-methoxy-3-{[(2S)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen-1- one;5-methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen- 1 -one;3-{[(2R)-1 -methyl pyrrolidin-2-yl](2H2)methyl}-5-(trifluoromethoxy)-2, 3-dihydro-1λ4- benzothiophen-1-one;5-(difluoromethoxy)-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1- one;5-(2H3)methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen- 1 -one;5-(2H3)methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]rnethyl}-2,3-dihydro-1λ4-benzothiophen-1-one;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(propan-2-yloxy)-2,3-dihydro-1λ4-benzothiophen-1- one;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(oxan-4-yloxy)-2,3-dihydro-1λ4-benzothiophen-1-one;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(oxan-4-yl)-2,3-dihydro-1λ4-benzothiophen-1-one;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(pyridin-4-yl)-2,3-dihydro-1λ4-benzothiophen-1 -one;5-(2-fluoropyridin-4-yl)-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2, 3-dihydro-1 λ4-benzothiophen- 1 -one;5-(4-fluorophenyl)-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1- one;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(thian-4-yl)-2,3-dihydro-1λ4-benzothiophen-1-one;4-(3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-1 -oxo-2, 3-dihydro-1 λ4-benzothiophen-5-yl )-1λ6- thiane-1 , 1-dione;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(1 -oxo-1 λ4-thian-4-yl)-2,3-dihydro-1 λ4-benzothiophen- 1 -one;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ4-benzothiophen-1-one;(3S)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ4-benzothiophen-1- one;(3R)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ4-benzothiophen-1 - one;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(1 ,2-thiazol-4-yl)-2,3-dihydro-1λ4-benzothiophen-1- one;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(1 , 3-thiazol-4-yl)-2,3-dihydro-1λ4-benzothiophen-1- one5-(2H3)methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4- benzothiophen-1-one;5-(cyclopropylmethoxy)-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4- benzothiophen-1-one;5-(cyclopropylmethoxy)-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4- benzothiophen-1-one;5-(cyclopropylmethoxy)-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen- 1 -one;5.6-dimethoxy-3-{[(2R)-pyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;5.6-dimethoxy-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1 -one;5.6-dimethoxy-3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1 - one;12-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-4,6-dioxa-10λ4-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8- trien-10-one;12-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-4,6-dioxa-10λ4-thiatricyclo[7.3.0.03,7]dodeca- 1 ,3(7),8-trien-10-one;4,5-dimethoxy-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;4-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;(3S)-4-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one; and(3R)-4-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

24. A compound according to claim 1 , wherein the compound is selected from:(3R)-4-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ4-benzothiophen-1-one;5-fluoro-3-{[(2R)-1 -methylpyrrolid in-2-yl]methyl}-2,3-dihydro- 1λ6-benzothiophene-1 ,1 -dione;(3S)-5-fluoro-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1 - dione;(3R)-5-fluoro-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1- dione;3-{[(2S)-1-methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1-dione;3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;3-{[(2S)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 , 1-dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro(4,5,6,7-2H4)-1λ6-benzothiophene-1,1- dione;3-{[(2R)-pyrrolidin-2-yl]methyl}-2,3-dihydro(4,5,6,7-2H4)-1λ6-benzothiophene-1,1-dione;3-{[(2R)-1-methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;5-methoxy-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;(3S)-5-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 λ6-benzothiophene-1 ,1 - dione;(3R)-5-methoxy-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1- dione;5-methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 λ6-benzothiophene-1 , 1 - dione;5-methoxy-3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;5-methoxy-3-{[(2S)-1-(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;5-methoxy-3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;3-{[(2R)-1-methylpyrrolidin-2-yl](2H2)methyl}-5-(trifluoromethoxy)-2,3-dihydro-1λ6- benzoth iophene- 1 ,1 -dione;5-(difluoromethoxy)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;5-(2H3)methoxy-3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;5-(2H3)methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1 λ6-benzothiophene-1 , 1 - dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yloxy)-2,3-dihydro-1λ6-benzothiophene-1,1- dione;3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-5-(oxan-4-yloxy)-2,3-dihydro-1 λ6-benzothiophene-1 , 1 - dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(oxan-4-yl)-2,3-dihydro-1λ6-benzothiophene-1,1- dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(pyridin-4-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1- dione;5-(2-fluoropyridin-4-yl)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;5-(4-fluorophenyl)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1- dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(thian-4-yl)-2,3-dihydro-1λ6-benzothiophene-1,1- dione;5-(1,1 -dioxo- 1λ6-thian-4-yl)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6- benzoth iophene-1 ,1 -dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(1-oxo-1λ4-thian-4-yl)-2,3-dihydro-1λ6- benzothiophene-1 ,1 -dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ6-benzothiophene-1,1- dione;(3S)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;(3R)-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(propan-2-yl)-2,3-dihydro-1λ6-benzothiophene-1,1 -dione;3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-(1,2-thiazol-4-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1- dione;3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-5-(1 ,3-thiazol-4-yl)-2,3-dihydro-1λ6-benzothiophene-1 ,1 - dione;5-(2H3)methoxy-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6- benzothiophene-1 ,1 -dione;5-(cyclopropylmethoxy)-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6- benzothiophene-1 ,1 -dione;5-(cyclopropylmethoxy)-3-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6- benzothiophene-1 ,1 -dione;5-(cyclopropylmethoxy)-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2, 3-dihydro-1λ6- benzothiophene-1 ,1 -dione;5.6-dimethoxy-3-{[(2R)-pyrrolidin-2-yl](2H2)methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1-dione;5.6-dimethoxy-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2, 3-dihydro-1 λ6-benzothiophene-1 , 1 - dione;5.6-dimethoxy-3-{[(2R)-1-(2H3)methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1-dione;12-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-4,6-dioxa-10λ6-thiatricyclo[7.3.0.03'7]dodeca-1 ,3(7),8- triene-10, 10-dione;12-{[(2R)-1 -(2H3)methylpyrrolidin-2-yl]methyl}-4,6-dioxa-10λ6-thiatricyclo[7.3.0.03,7]dodeca-1 ,3(7),8-triene-10, 10-dione;4, 5-dimethoxy-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2, 3-dihydro-1 λ6-benzothiophene-1 , 1 - dione;4-methoxy-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1 ,1 -dione;(3S)-4-methoxy-3-{[(2R)-1 -methyl pyrrolidin-2-yl]methyl}-2, 3-dihydro-1 λ6-benzothiophene-1 , 1- dione; and(3R)-4-methoxy-3-{[(2R)-1 -methylpyrrolidin-2-yl]methyl}-2,3-dihydro-1λ6-benzothiophene-1,1- dione, or a pharmaceutically acceptable salt, solvate, and / or prodrug thereof.

25. A composition comprising one or more compounds of any one of claims 1 to 24 and a carrier.

26. A method of treating depressive disorder, bipolar disorder, eating disorder, impulse control disorder, personality disorder, substance abuse disorder, behavioral addiction disorder, anxiety disorder, stress disorder, neurodevelopmental disorder, pain disorder, headache disorder, inflammatory disorder, injury-related disorder, neurodegenerative disorder, functional disorder, psychotic disorder, hyperkinetic movement disorder, age-related macular degeneration, atherosclerosis, dissociative disorders, genetic brain disorders, hyperprolactinemia, hypersomnia, obesity, phobias, apathy disorders, and / or burnout comprising administering a therapeutically effective amount of one or more compounds of any one of claims 1 to 24 or the composition of claim 25 to a subject in need thereof.